Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
155491018 173511 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
44453327 94652 18 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 94652 18 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
10585 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
69212799 77622 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77622 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
508750 167970 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 167970 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
10585 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
44395055 64173 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64173 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
73351183 92802 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 92802 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
70697571 77621 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77621 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
11735999 188761 0 None - 1 Human 10.4 pED50 = 10.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512607 188761 0 None - 1 Human 10.4 pED50 = 10.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11322108 177992 0 None - 1 Human 10.2 pED50 = 10.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467070 177992 0 None - 1 Human 10.2 pED50 = 10.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11254190 188763 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512615 188763 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11651747 173197 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
CHEMBL453720 173197 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
11659300 178187 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL468733 178187 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11151928 188897 0 None 1 4 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL513863 188897 0 None 1 4 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11173161 188220 0 None - 0 Human 9.7 pED50 = 9.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL506023 188220 0 None - 0 Human 9.7 pED50 = 9.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157844 188700 0 None - 1 Human 9.4 pED50 = 9.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL512094 188700 0 None - 1 Human 9.4 pED50 = 9.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11218678 169785 0 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL444736 169785 0 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11543222 192857 3 None - 0 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
CHEMBL526704 192857 3 None - 0 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
11536008 178019 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
CHEMBL467276 178019 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
11551248 178084 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467685 178084 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11390777 172047 0 None - 0 Human 9.0 pED50 = 9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL449215 172047 0 None - 0 Human 9.0 pED50 = 9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11198073 177904 0 None - 1 Human 8.0 pED50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466434 177904 0 None - 1 Human 8.0 pED50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11370332 62966 0 None - 1 Human 7.8 pED50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL179312 62966 0 None - 1 Human 7.8 pED50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 177902 0 None - 1 Human 6.7 pED50 = 6.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 177902 0 None - 1 Human 6.7 pED50 = 6.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 177902 0 None - 1 Human 8.5 pED50 = 8.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 177902 0 None - 1 Human 8.5 pED50 = 8.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11151929 178186 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468732 178186 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11359715 178185 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468720 178185 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
11544064 177903 0 None - 1 Human 8.3 pED50 = 8.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
CHEMBL466433 177903 0 None - 1 Human 8.3 pED50 = 8.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
11609693 188623 0 None - 0 Human 8.2 pED50 = 8.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
CHEMBL511426 188623 0 None - 0 Human 8.2 pED50 = 8.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
11437477 188039 0 None - 1 Human 8.1 pED50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL502976 188039 0 None - 1 Human 8.1 pED50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44593562 186912 0 None - 1 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 1 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
86642531 137775 0 None 10 2 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 137775 0 None 10 2 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
44425645 85655 0 None 7 2 Human 9.8 pIC50 = 9.8 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 85655 0 None 7 2 Human 9.8 pIC50 = 9.8 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240064 187844 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 187844 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593562 186912 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425652 168203 0 None 12 2 Human 9.6 pIC50 = 9.6 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168203 0 None 12 2 Human 9.6 pIC50 = 9.6 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10289827 187393 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187393 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593563 192508 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 192508 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425647 85674 0 None 5 2 Human 9.5 pIC50 = 9.5 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 85674 0 None 5 2 Human 9.5 pIC50 = 9.5 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425292 85541 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85541 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85541 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85541 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
10240064 187844 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 187844 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46865775 8030 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8030 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
24801689 97345 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97345 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425255 168318 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168318 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425652 168203 0 None 12 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168203 0 None 12 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
59370257 137636 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769444 137636 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
10129192 187875 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 187875 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11598 666 6 None 891 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
23725177 666 6 None 891 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4442783 666 6 None 891 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
44425254 141728 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 141728 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 152995 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 152995 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425645 85655 0 None 7 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 85655 0 None 7 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11597 667 3 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 667 3 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 667 3 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
51039119 175643 29 None -1 3 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 175643 29 None -1 3 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
44593564 186649 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 186649 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
25022597 94895 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 94895 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44453440 97239 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97239 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
183790 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
183790 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3685 8 None -1 4 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
24801690 97591 19 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 97591 19 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57402219 70664 0 None 52 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 70664 0 None 52 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
24801690 97591 19 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44593564 186649 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 186649 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44573649 186652 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 186652 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
44593562 186912 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10175425 192860 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 192860 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
127025088 137735 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770530 137735 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
127025086 137655 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769610 137655 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46865774 8029 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8029 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
86642531 137775 0 None -10 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 137775 0 None -10 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
10007642 18917 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 18917 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10218403 187327 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187327 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
46886055 7962 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 7962 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025093 137686 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769984 137686 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46830335 8131 4 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8131 4 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
11365166 74195 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74195 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
52941377 19133 0 None 7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19133 0 None 7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
16216716 152995 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 152995 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85541 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85541 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 152995 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 152995 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11353855 74200 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74200 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44425652 168203 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168203 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425652 168203 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168203 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
57335017 69995 0 None 1380 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 69995 0 None 1380 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
70691785 73379 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73379 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
46830336 7768 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7768 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
54754967 77477 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77477 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
10239991 187863 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 187863 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391766 70673 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 70673 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
10187492 147257 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147257 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25256791 187108 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187108 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
11502371 152594 1 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 152594 1 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11502371 152594 1 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 152594 1 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10154434 58481 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
CHEMBL1687955 58481 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
44413167 79309 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211560 79309 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9967878 84655 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
CHEMBL224510 84655 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
44421867 84733 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
CHEMBL225166 84733 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
44421889 84795 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225582 84795 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098519 84806 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225637 84806 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098523 141757 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL388516 141757 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421913 161336 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
CHEMBL415061 161336 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
21098488 165714 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL426925 165714 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098490 165772 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL427245 165772 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421917 165774 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL427254 165774 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
9840006 141494 5 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL387625 141494 5 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
9956238 59882 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 59882 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 59882 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
44453002 154834 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403424 154834 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44421860 84624 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224166 84624 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9900683 141380 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL386937 141380 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
10065796 141535 4 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL387954 141535 4 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54585109 62244 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62244 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
44453234 97022 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97022 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
22143196 183405 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183405 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143196 183405 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183405 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44416138 138345 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138345 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46927117 65097 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65097 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
44453405 94992 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 94992 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
44453407 94993 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 94993 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
56675205 65464 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65464 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56671793 65465 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65465 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671795 65468 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65468 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
46884856 8260 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8260 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
44583280 171883 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 171883 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
46885159 8290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
46885160 8291 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093154 8291 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
9974356 137066 4 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL375556 137066 4 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
57396726 68613 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922817 68613 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
44439163 89863 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 89863 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
183790 3685 8 None -1 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
783 3685 8 None -1 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
CHEMBL1178786 3685 8 None -1 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
11283842 73390 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73390 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11353855 74200 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74200 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56643545 68618 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68618 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
52943756 19094 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19094 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44453368 97318 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97318 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
56683116 65475 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65475 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
46884898 7636 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7636 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
44453409 94995 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 94995 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22143146 183324 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183324 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
10218843 172217 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172217 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425641 85639 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 85639 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
10007642 18917 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 18917 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
46885028 8337 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8337 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
24801523 97406 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97406 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
57656833 74879 0 None -257 4 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None -257 4 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
122181148 121322 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589843 121322 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
9956238 59882 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 59882 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 59882 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
508742 95132 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95132 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
145963552 160801 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4125866 160801 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
122181146 121320 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121320 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44447435 94258 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94258 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447435 94258 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94258 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145962429 161021 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
CHEMBL4128975 161021 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
44453538 97481 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97481 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
46240482 83164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83164 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
22143294 192823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 192823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44580590 192866 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 192866 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
70683350 73378 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73378 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
44425641 85639 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 85639 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425288 85588 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 85588 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 142835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 142835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
69035677 77296 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77296 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
44425288 85588 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 85588 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 142835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 142835 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44571218 183296 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183296 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57344310 68594 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922794 68594 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57343820 68612 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922816 68612 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
24801525 97160 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97160 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
49763686 65093 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65093 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57396724 68605 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922805 68605 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57396725 68607 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922808 68607 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563039 191447 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL520228 191447 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11179439 73388 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73388 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46947816 65102 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65102 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
44563113 174011 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455682 174011 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
508877 94618 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 94618 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
54756045 65457 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65457 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678507 65469 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65469 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447429 94206 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94206 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50925394 19132 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19132 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44447429 94206 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94206 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425286 152713 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 152713 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425286 152713 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 152713 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
57344299 68614 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922818 68614 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
56669631 65478 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65478 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
132572938 156248 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156248 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44439158 146294 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146294 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
10272003 58571 1 None -2 3 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58571 1 None -2 3 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
57403700 68603 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922803 68603 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10427217 84573 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL223815 84573 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
10041590 141579 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL388285 141579 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54584164 62239 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62239 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44595711 136797 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 136797 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
49763568 65084 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65084 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
11752457 74190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
54755081 65446 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65446 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671794 65466 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65466 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425634 141486 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 141486 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44442599 93216 0 None 31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93216 0 None 31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10291634 58569 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
CHEMBL1688879 58569 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
10154979 58570 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
CHEMBL1688880 58570 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
10064487 84593 4 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223907 84593 4 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
11585168 90257 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90257 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57402219 70664 0 None -52 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 70664 0 None -52 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
145961260 160884 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127096 160884 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
52941377 19133 0 None -7 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19133 0 None -7 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
57394970 68601 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922800 68601 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
44583282 172126 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172126 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
53389660 170917 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 170917 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389845 172392 0 None 45 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172392 0 None 45 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
57344303 68589 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922789 68589 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44353447 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
44425634 141486 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 141486 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11192346 1993 50 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
44583281 187652 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 187652 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
49763575 65114 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65114 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
24801522 160590 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 160590 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
46884855 8219 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8219 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
122181235 121336 0 None 5 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121336 0 None 5 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
9923015 58568 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
CHEMBL1688878 58568 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
11582651 74853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 74853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
145961759 160983 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
CHEMBL4128487 160983 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
57656921 74863 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 74863 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
122181152 121192 0 None 25 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121192 0 None 25 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
46241610 83157 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83157 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
122181238 121339 0 None 194 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121339 0 None 194 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
10304021 73372 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73372 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
11504634 185454 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487070 185454 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
56678508 65470 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65470 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44570718 183251 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183251 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44580590 192866 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 192866 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
46944853 65099 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65099 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
49763574 65113 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65113 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755083 65413 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65413 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
46885029 8165 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8165 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
10315045 143043 5 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL389926 143043 5 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
122181153 121326 0 None 20 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121326 0 None 20 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
44416274 158008 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL409162 158008 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10346048 77853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 77853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145962546 160863 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126779 160863 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11553070 74850 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 74850 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10346048 77853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 77853 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
11563451 151386 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151386 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
24801690 97591 19 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 97591 19 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
70689914 74203 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74203 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
24801690 97591 19 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44453366 157759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 157759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
46885027 8336 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8336 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53322810 58164 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58164 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54585107 62232 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62232 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54580188 62238 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62238 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53325639 58162 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58162 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181147 121321 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589842 121321 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
11670910 88194 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL235657 88194 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
145961961 160949 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128015 160949 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
57656640 74861 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 74861 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
44439155 91542 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91542 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885269 7821 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1090148 7821 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
56643545 68618 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68618 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57398494 68616 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922820 68616 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
22143104 187475 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 187475 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
22143294 192823 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 192823 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44571257 190500 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 190500 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11192346 1993 50 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
56661444 65444 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65444 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425637 85560 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85560 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425637 85560 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85560 0 None 3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425629 85599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 85599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44442593 146667 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 146667 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
57344218 68606 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922806 68606 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563038 185457 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487074 185457 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
21098512 84665 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224594 84665 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098530 143027 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL389915 143027 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44447426 94172 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94172 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145961667 160807 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126007 160807 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
44447426 94172 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94172 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145963369 160839 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126360 160839 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
11548199 89492 0 None 707 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89492 0 None 707 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
22143255 187275 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187275 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143155 187479 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 187479 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44593555 188198 0 None 2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188198 0 None 2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570714 189202 0 None 9 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189202 0 None 9 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
9850318 94801 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 94801 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
10392978 166899 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 166899 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
54754968 65411 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65411 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425647 85674 0 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 85674 0 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423283 84883 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 84883 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44583283 187702 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 187702 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
127026243 137741 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770591 137741 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
53321616 58152 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58152 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11433008 77284 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77284 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10289827 187393 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187393 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
25110716 154667 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 154667 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
53318853 58148 0 None 27 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58148 0 None 27 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
11597 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
11387511 74192 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74192 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44453441 97240 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97240 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
46885213 8375 0 None 52 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8375 0 None 52 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
57391767 70675 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 70675 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
127029034 137687 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770008 137687 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
11192346 1993 50 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None -1 3 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10300284 73384 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73384 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57396998 70670 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 70670 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
54755919 65428 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65428 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
54755801 65429 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65429 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56659295 65479 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65479 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425629 85599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 85599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 59882 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 59882 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 59882 1 None 3 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
57656833 74879 0 None -42 4 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None -42 4 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44421923 84658 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224535 84658 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
9857714 84707 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224885 84707 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421855 84690 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224746 84690 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
11723420 136028 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL373759 136028 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
57656887 74862 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 74862 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447427 154309 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154309 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447427 154309 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154309 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
11570431 91550 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91550 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
22143346 172082 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172082 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
10175423 187862 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 187862 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
10312346 187878 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 187878 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
10152864 187291 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187291 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
49763931 65095 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65095 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
44453330 95058 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95058 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
44453300 96986 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 96986 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44416274 158008 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL409162 158008 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
24801523 97406 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97406 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
10458152 77448 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77448 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10458152 77448 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77448 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
49764446 65109 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65109 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44453474 97422 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97422 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56659196 65472 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65472 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
22143258 183297 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183297 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57656942 74689 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 74689 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57403699 68595 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922795 68595 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453004 94820 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL256256 94820 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10471319 84379 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223336 84379 5 None - 1 Human 4.7 pIC50 = 4.7 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44439169 90343 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90343 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44447446 154340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL400724 154340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44447424 94171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447446 154340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL400724 154340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11306757 73389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11489078 73457 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73457 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44570781 191966 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 191966 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
46830335 8131 4 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8131 4 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46842383 8261 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8261 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
70689915 74204 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74204 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
44453472 154998 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 154998 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
54586021 62214 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62214 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
57396723 68604 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922804 68604 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10360623 84782 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL225492 84782 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44447424 94171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44583280 171883 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 171883 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
10281316 73374 0 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73374 0 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
44453327 94652 18 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 94652 18 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10162782 73358 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73358 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44442590 93339 0 None 169 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93339 0 None 169 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
49763804 65094 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65094 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
11510932 74852 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 74852 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
145962732 160810 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126032 160810 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44580591 187276 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187276 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
49763682 65090 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65090 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44447432 154310 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154310 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44447432 154310 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154310 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50991056 62237 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62237 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57394966 68585 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922785 68585 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
145953092 160791 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4125768 160791 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143309 187358 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187358 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
10111333 174894 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 174894 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10142792 93308 0 None 26 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93308 0 None 26 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
57656869 74871 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 74871 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
52943756 19094 0 None -23 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19094 0 None -23 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
49764196 65111 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65111 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44570717 183250 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183250 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
56676474 65481 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65481 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
183790 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
783 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
CHEMBL1178786 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
44425309 141825 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 141825 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
183790 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
783 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
CHEMBL1178786 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
183790 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -1 4 Human 7.6 pIC50 = 7.6 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22143334 187225 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187225 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57344297 68611 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922815 68611 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
11711078 74870 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 74870 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83167 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83167 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
46944854 65098 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65098 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54756156 65454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65454 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447431 94233 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94233 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 141814 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 141814 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44447431 94233 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94233 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 141814 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 141814 0 None 12 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11678573 90208 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90208 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57656713 74855 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 74855 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447433 94256 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94256 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44447433 94256 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94256 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
22143293 187444 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 187444 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44447434 94257 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94257 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44453535 154635 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 154635 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
44447434 94257 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94257 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
155521447 170017 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170017 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
11227168 74201 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74201 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
46884818 7789 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7789 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
145963669 161011 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128832 161011 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44416157 80183 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80183 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143309 187358 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187358 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
22143112 187861 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 187861 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
57395219 70667 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 70667 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
11756884 18898 0 None 25 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 18898 0 None 25 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
54754969 65409 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65409 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44425645 85655 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 85655 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44453442 97241 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97241 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425645 85655 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 85655 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395217 70665 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 70665 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
50992246 58163 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58163 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
50992246 58163 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58163 2 None -1 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44593561 12554 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12554 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12554 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
11192346 1993 50 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None 1 3 Human 8.5 pIC50 = 8.5 Functional
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
67011331 74196 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74196 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425653 85802 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 85802 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 152997 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 152997 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11627639 94492 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94492 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44425653 85802 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 85802 0 None 4 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 152997 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 152997 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44453472 154998 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 154998 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
24801689 97345 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97345 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
46830336 7768 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7768 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11421712 74194 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74194 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10008367 1991 43 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 1991 43 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 1991 43 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 1991 43 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425647 85674 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 85674 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395218 70666 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 70666 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
11192346 1993 50 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
50992246 58163 2 None -1 5 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58163 2 None -1 5 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
508869 94996 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 94996 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425647 85674 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 85674 0 None 5 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425643 85615 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 85615 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
46241717 83154 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83154 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46208367 83168 8 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83168 8 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
24801522 160590 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 160590 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
56657929 65461 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65461 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
46842383 8261 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8261 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44425308 153172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL398150 153172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
10111333 174894 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 174894 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44425308 153172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL398150 153172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
54585107 62232 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62232 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44353447 3716 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3716 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3716 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
137654404 158023 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4091736 158023 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
44421922 144017 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390736 144017 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9836178 84653 2 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224500 84653 2 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
10245340 168371 5 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL438783 168371 5 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
67011331 74196 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74196 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57656657 74859 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 74859 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56671792 65463 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65463 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
162666730 181692 0 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
122181149 121323 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589844 121323 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
11534473 90268 0 None 117 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90268 0 None 117 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
10117480 73368 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73368 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
70688149 74874 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 74874 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44296219 100844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
CHEMBL296609 100844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
44442598 153853 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 153853 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
71452241 83155 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83155 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
10120067 73381 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73381 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
70689914 74203 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74203 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
70689915 74204 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74204 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
162666730 181692 0 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None 562 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
56659197 65473 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65473 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
22725647 173127 0 None 52 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173127 0 None 52 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155521447 170017 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170017 0 None 3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
145954949 161095 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4130191 161095 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10129343 172694 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 172694 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
56668309 65445 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65445 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
54756038 65447 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65447 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
49763571 65087 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65087 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
46945254 65104 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65104 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
57344305 68597 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922797 68597 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453373 97362 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97362 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
54755079 65410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
3547 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL38380 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL541388 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
3547 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL38380 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL541388 140841 67 None - 1 Human 4.5 pIC50 = 4.5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
122181236 121337 0 None 13 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121337 0 None 13 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
11319072 74193 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74193 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57344296 68609 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922813 68609 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
23630215 62215 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62215 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44453134 97614 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 97614 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
67220645 74880 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 74880 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453298 154700 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 154700 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44442599 93216 0 None 31 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93216 0 None 31 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11353843 74198 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74198 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56683121 65480 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65480 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
10196988 168898 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 168898 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57401954 68617 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922822 68617 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57656854 74878 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 74878 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
22143255 187275 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187275 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10323427 79350 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79350 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
145953765 160978 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128372 160978 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44442587 93376 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93376 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10323427 79350 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79350 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
10129343 172694 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 172694 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
145962575 160921 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127580 160921 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10268598 58567 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
CHEMBL1688877 58567 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
10436083 79467 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79467 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44415880 168773 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 168773 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46241010 83171 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83171 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56643545 68618 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68618 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10281316 73374 0 None 2 3 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73374 0 None 2 3 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
25154827 174012 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455683 174012 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
56657930 65462 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65462 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
44425643 85615 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 85615 0 None 14 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10120907 73376 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73376 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
11227168 74201 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74201 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11527661 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11527661 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 1990 25 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
22143346 172082 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172082 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
11753466 77287 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77287 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
51039119 175643 29 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 175643 29 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
24801526 97167 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97167 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
11330837 74202 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74202 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56671925 65418 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65418 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
22725647 173127 0 None 52 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173127 0 None 52 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
54582215 62231 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62231 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10436083 79467 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79467 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9858433 84654 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224509 84654 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
127025091 137682 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
CHEMBL3769934 137682 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
22143305 183030 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183030 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425306 141837 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL388949 141837 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44453592 159508 20 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 159508 20 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44453565 168441 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 168441 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
49764447 65091 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65091 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
24801525 97160 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97160 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
11598084 74854 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 74854 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 74872 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 74872 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44425306 141837 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL388949 141837 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
57656749 74860 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 74860 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44413147 139183 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139183 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
44413147 139183 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139183 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
46241718 83158 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83158 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
44453471 97421 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97421 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44453562 155114 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155114 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10312346 187878 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 187878 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
54581190 62233 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62233 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
70696470 74868 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 74868 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
46241608 83156 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83156 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
11756884 18898 0 None -25 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 18898 0 None -25 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
508729 95091 1 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95091 1 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
145963612 160892 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
CHEMBL4127249 160892 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
54582216 62236 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62236 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583186 62243 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62243 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181151 121325 0 None 7 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121325 0 None 7 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
54754722 65421 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65421 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453171 95293 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95293 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
57344221 68615 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922819 68615 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
145955877 160857 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126634 160857 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143334 187225 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187225 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10209478 73373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
11591776 144953 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL391459 144953 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
10239991 187863 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 187863 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593555 188198 0 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188198 0 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453408 94994 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 94994 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44573608 186968 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 186968 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10167417 73377 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73377 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44453440 97239 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97239 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425293 152930 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 152930 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143155 187479 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 187479 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
11330529 74191 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74191 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22143146 183324 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183324 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453298 154700 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 154700 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
57396999 70674 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 70674 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
11192943 77271 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77271 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
53322809 58149 0 None 13 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58149 0 None 13 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
57391765 70671 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 70671 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
69035439 77295 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77295 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
57656833 74879 0 None 4 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None 4 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10323427 79350 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79350 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
57400160 68583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922783 68583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
54584109 62218 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62218 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44421868 84734 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL225167 84734 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098480 143611 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390389 143611 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145962604 160980 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128399 160980 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11180383 77270 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77270 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143200 187182 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187182 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
44442586 93378 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93378 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10164316 154254 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154254 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56667036 65096 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65096 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
56677288 65112 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65112 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
11409228 74185 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74185 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
46842084 7833 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7833 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
57396722 68602 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922801 68602 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
11721085 166306 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166306 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353447 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
46927116 65106 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65106 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57656871 74877 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 74877 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
145962608 160986 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128514 160986 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
46241509 83149 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83149 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
44423283 84883 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 84883 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44442587 93376 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93376 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
46944855 65103 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65103 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44416273 138412 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138412 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44416273 138412 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138412 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
57656938 74865 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 74865 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44442590 93339 0 None 169 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93339 0 None 169 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 146667 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 146667 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11647276 74857 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 74857 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
70681778 74867 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 74867 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
11690139 74875 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 74875 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57656719 74866 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 74866 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56643545 68618 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68618 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44580591 187276 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187276 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44571218 183296 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183296 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143258 183297 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183297 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11584094 188345 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508015 188345 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11613399 188358 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508073 188358 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11527661 1990 25 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 1990 25 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 1990 25 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11353843 74198 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74198 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453329 154812 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 154812 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
53325639 58162 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58162 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
54583111 62216 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62216 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44583281 187652 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 187652 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
11421712 74194 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74194 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
50925394 19132 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19132 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53324304 58156 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58156 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
46240484 83166 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83166 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
57394969 68598 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922798 68598 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44421888 84769 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225434 84769 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
44421862 135857 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL373512 135857 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145961982 160985 0 None 10 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128498 160985 0 None 10 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
122181237 121338 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589951 121338 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
46842232 7800 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7800 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
11567495 74849 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 74849 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
24801526 97167 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97167 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
145953762 160887 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4127135 160887 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
10240278 172328 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172328 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
57344298 68610 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922814 68610 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453409 94995 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 94995 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656715 74856 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 74856 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57344315 68599 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
CHEMBL1922799 68599 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
44447436 154154 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154154 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447436 154154 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154154 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
46240785 83169 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83169 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
23630215 62215 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62215 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
54754724 65423 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65423 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54580190 62242 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62242 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46842235 7754 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7754 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
49764322 65110 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65110 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11365166 74195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
135981707 65459 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65459 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44425654 85803 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 85803 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425654 85803 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 85803 0 None 2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57344316 68592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922792 68592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
46240687 83172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44439166 90115 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90115 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
122181144 121318 0 None 35 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121318 0 None 35 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
10182382 93528 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93528 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
22143293 187444 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 187444 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44583282 172126 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172126 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
22143241 182668 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 182668 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
56643545 68618 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68618 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
11591595 185575 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487238 185575 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
54755560 65448 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65448 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56661451 65467 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65467 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56683044 65471 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65471 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56662695 65474 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65474 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
10232019 73382 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73382 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
57398750 70672 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 70672 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
127025092 137695 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770125 137695 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
10152864 187291 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187291 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391768 70669 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 70669 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
25022597 94895 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 94895 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44425633 85614 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 85614 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425633 85614 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 85614 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
50991056 62237 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62237 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10008367 1991 43 None -2 3 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 1991 43 None -2 3 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 1991 43 None -2 3 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 1991 43 None -2 3 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425635 152998 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 152998 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
46240585 83170 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83170 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44353447 3716 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3716 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3716 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
10272003 58571 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58571 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
10272003 58571 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58571 1 None 2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
21098469 141820 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL388742 141820 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
54585108 62234 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62234 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583187 62245 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62245 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
46885214 7617 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1088810 7617 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
145960485 161003 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4128742 161003 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
44442586 93378 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93378 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
54583112 62217 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62217 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46241826 83148 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83148 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
145954490 161086 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4130047 161086 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
70693849 73383 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73383 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
44453507 168412 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168412 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
54583185 62235 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62235 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57393249 68619 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C\c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922824 68619 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C\c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
22143196 183405 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183405 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143196 183405 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183405 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57656825 74858 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 74858 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842086 7897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
122181145 121319 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121319 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44413411 77385 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77385 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44413411 77385 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77385 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44453534 97432 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97432 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
44413144 138689 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 138689 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
44413144 138689 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 138689 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145960924 160997 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128658 160997 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
162658125 180514 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57335017 69995 0 None 1380 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 69995 0 None 1380 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10142792 93308 0 None 26 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93308 0 None 26 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143112 187861 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 187861 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
22143305 183030 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183030 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570781 191966 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 191966 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
56664979 65412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425635 152998 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 152998 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11421840 77285 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77285 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
11273379 74199 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74199 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453365 97078 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97078 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
53322810 58164 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58164 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425630 85600 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 85600 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
9956238 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 59882 1 None 3 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
21098478 142108 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL389168 142108 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098468 144140 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL390837 144140 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
68616341 73385 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73385 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57400161 68584 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922784 68584 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44442598 153853 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 153853 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11843812 79494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11606702 145221 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145221 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344307 68596 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922796 68596 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413399 79119 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79119 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11843812 79494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44413399 79119 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79119 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10187492 147257 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147257 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
54754723 65422 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65422 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57394967 68586 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922786 68586 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413137 78482 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78482 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
162658125 180514 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None 100 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44425308 153172 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL398150 153172 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44413137 78482 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78482 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
155514261 169269 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169269 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169269 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169269 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
11273379 74199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
122181150 121324 0 None 125 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121324 0 None 125 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
781 3344 71 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10165625 73380 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73380 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
46884898 7636 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7636 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46885027 8336 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8336 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53325460 58186 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58186 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
56671923 65408 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65408 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44425630 85600 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 85600 0 None 14 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
127025089 137777 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770951 137777 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
44453325 155001 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155001 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
57395216 70668 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 70668 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
44453372 155203 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155203 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
10281715 73375 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73375 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
54582217 62241 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62241 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57344314 68588 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922788 68588 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57394968 68587 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922787 68587 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
57391487 68593 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922793 68593 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
70692344 74848 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 74848 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
57398493 68608 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922811 68608 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563071 186113 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL488433 186113 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
11632418 74847 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 74847 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415898 80709 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 80709 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44415898 80709 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 80709 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
57344317 68590 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922790 68590 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57344318 68591 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922791 68591 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453327 94652 18 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 94652 18 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
57393497 68790 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 68790 0 None - 0 Human 6.0 pKd = 6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
15985912 83561 0 None - 0 Human 5.0 pKd = 5 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83561 0 None - 0 Human 5.0 pKd = 5 Functional
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57400128 68783 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 68783 0 None - 0 Human 5.9 pKd = 5.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400125 68772 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 68772 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44180522 68792 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 68792 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393496 68789 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 68789 0 None - 0 Human 5.6 pKd = 5.6 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57656833 74879 0 None 4 4 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None 4 4 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57393219 68780 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 68780 0 None - 0 Human 5.5 pKd = 5.5 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400127 68782 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 68782 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 68784 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 68784 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57397001 68786 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 68786 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400420 68787 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 68787 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57393495 68788 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 68788 0 None - 0 Human 5.4 pKd = 5.4 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400129 68785 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 68785 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57395221 68791 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 68791 0 None - 0 Human 6.3 pKd = 6.3 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57398458 68781 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 68781 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
16124598 10629 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171008 10629 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798435 10603 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170828 10603 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798434 10602 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170827 10602 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798461 10593 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170725 10593 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
17756652 10630 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171011 10630 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798461 10593 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10593 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57398458 68781 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 68781 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 68784 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 68784 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
15985914 83560 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83560 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985914 83560 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83560 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83561 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83561 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57394938 68776 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 68776 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
57394938 68776 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 68776 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
49798291 10457 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10457 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798289 10550 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10550 0 None - 0 Mouse 6.0 pKi = 6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798289 10550 0 None - 0 Human 5.0 pKi = 5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10550 0 None - 0 Human 5.0 pKi = 5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798462 10496 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169994 10496 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296310 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL49994 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296310 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296310 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 187685 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798289 10550 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10550 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
9870980 154110 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154110 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
49798265 10628 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10628 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798461 10593 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10593 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57393218 68775 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 68775 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
9870980 154110 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154110 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296287 101217 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL299379 101217 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
57400125 68772 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 68772 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 68773 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 68773 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296265 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53131 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296265 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296265 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 192997 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798463 10497 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
CHEMBL1169995 10497 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
49798289 10550 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10550 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798347 10475 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169824 10475 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
49798323 10688 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10688 0 None - 0 Mouse 6.8 pKi = 6.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
19430534 10672 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10672 0 None - 0 Mouse 5.8 pKi = 5.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57396690 68778 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 68778 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57400128 68783 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 68783 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
44296501 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL300025 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
44296501 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296501 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101316 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296264 192996 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53130 192996 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44446951 94167 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94167 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44446951 94167 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94167 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798438 10592 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170722 10592 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798323 10688 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10688 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798464 10529 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170187 10529 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798264 10687 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10687 0 None - 0 Mouse 5.7 pKi = 5.7 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400129 68785 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 68785 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400125 68772 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 68772 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57391450 68777 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 68777 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296268 101373 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300455 101373 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
57393496 68789 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 68789 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393497 68790 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 68790 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
49798437 10459 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169660 10459 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296155 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297950 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296155 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57391449 68774 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 68774 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798264 10687 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10687 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798292 10458 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10458 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798265 10628 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10628 0 None - 0 Mouse 6.6 pKi = 6.6 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57391450 68777 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 68777 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296155 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101032 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57394939 68779 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 68779 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
44296269 193067 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53557 193067 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296269 193067 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53557 193067 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296287 101217 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL299379 101217 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
57400127 68782 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 68782 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
49798436 10604 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170829 10604 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
49798349 10691 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171786 10691 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798399 10600 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170801 10600 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798265 10628 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10628 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110660 94355 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94355 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
25110660 94355 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94355 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296630 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297033 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296630 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296630 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 100895 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296366 188836 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51332 188836 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
44296384 193264 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL54192 193264 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
49798292 10458 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10458 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10687 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10687 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10687 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10687 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798397 10598 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170799 10598 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798351 10693 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
CHEMBL1171788 10693 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
49798325 10705 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10705 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400420 68787 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 68787 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57391449 68774 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 68774 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296087 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299153 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296087 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296344 162004 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
CHEMBL416833 162004 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
44296087 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101185 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53779 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296409 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53930 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296469 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 193090 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 193158 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299322 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296629 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101209 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798350 10692 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
CHEMBL1171787 10692 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
10436045 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
782 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
CHEMBL432713 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
10436045 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798398 10599 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170800 10599 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798489 10633 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171035 10633 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
10436045 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3460 3 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798325 10705 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10705 0 None - 0 Mouse 6.3 pKi = 6.3 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110679 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL433081 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
25110679 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
25110679 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 167589 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296428 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299855 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296428 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296428 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101291 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
25110564 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
25110564 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 193105 0 None - 0 Human 5.3 pKi = 5.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
44296398 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL50025 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296398 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53476 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296410 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296398 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 187706 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 193052 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
10940216 190614 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL51895 190614 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
44296077 101414 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300744 101414 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296077 101414 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL300744 101414 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44180522 68792 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 68792 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393219 68780 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 68780 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57393495 68788 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 68788 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 68773 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 68773 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798265 10628 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10628 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798291 10457 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10457 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798326 10646 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10646 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
49798326 10646 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10646 0 None - 0 Mouse 6.2 pKi = 6.2 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
44296309 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50301 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296309 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296309 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188043 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
9870980 202582 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 202582 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57394939 68779 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 68779 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
9870980 202582 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 202582 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296154 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51094 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296154 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296154 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 188565 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798348 10675 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171614 10675 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
25110678 192950 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL52956 192950 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
25110678 192950 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 192950 0 None - 0 Human 5.2 pKi = 5.2 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
25110678 192950 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 192950 0 None - 0 Human 5.1 pKi = 5.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
44296137 101105 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL298562 101105 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
25110660 154333 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154333 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57393218 68775 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 68775 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
15985912 83561 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83561 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
25110660 154333 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154333 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296628 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50460 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296266 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
CHEMBL53991 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
44296628 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57396690 68778 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 68778 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
49798396 10658 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171398 10658 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
19430534 10672 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10672 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
44296628 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188129 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 193184 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57397001 68786 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 68786 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57395221 68791 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 68791 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
44296429 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53402 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296429 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296429 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 193039 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
8921 3089 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Calculated from ng/ml based on a mol weight of ~150kDa.Calculated from ng/ml based on a mol weight of ~150kDa.
Guide to Pharmacology None None None None None
11185 1960 31 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
25134303 1960 31 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
CHEMBL2178573 1960 31 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
DB16066 1960 31 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
769 813 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
769 813 0 None -28 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
11192346 1993 50 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
9032 1993 50 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
CHEMBL2029422 1993 50 None 1 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
11527661 1990 25 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
9045 1990 25 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
CHEMBL1963131 1990 25 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
776 840 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
759 854 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
759 854 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
759 854 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
11597 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
23725180 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
CHEMBL4781426 667 3 None 11 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
46213922 541 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
57656761 541 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
7825 541 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
772 857 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 815 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 815 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
68764898 665 1 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
9430 665 1 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
CHEMBL3577945 665 1 None 3 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
771 825 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10770925
771 825 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
771 825 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
771 825 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
771 825 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
775 837 0 None -316 2 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
10000456 3337 26 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
779 3337 26 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
CHEMBL1593104 3337 26 None 1 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
774 3914 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
10008367 1991 43 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
777 1991 43 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL1289316 1991 43 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL2426341 1991 43 None -2 3 Mouse 8.0 pIC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
773 1906 0 None 12 2 Human 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9789057
5071702 3340 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
780 3340 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
778 2433 0 None - 1 Human 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600978
486830 3939 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217
768 3939 0 None 6 5 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
183790 3685 8 None -3 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3685 8 None -3 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3685 8 None -3 2 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3088 99 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3088 99 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3088 99 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3088 99 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3088 99 None - 1 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
183790 3685 8 None -3 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3685 8 None -3 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3685 8 None -3 2 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3088 99 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3088 99 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3088 99 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3088 99 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3088 99 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
68767577 109328 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109328 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
68988296 109330 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109330 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11627840 95255 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258205 95255 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
68764898 665 1 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 665 1 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 665 1 None - 3 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
183790 3685 8 None -3 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3685 8 None -3 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3685 8 None -3 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
90656027 110638 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263286 110638 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
91884571 180878 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 180878 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
46886055 7962 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 7962 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
68767577 109328 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109328 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
10289827 187393 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187393 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46886536 8222 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092678 8222 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
154572822 170535 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4457723 170535 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
16064151 120726 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577948 120726 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
44425292 85541 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85541 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
68764925 120724 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 120724 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
46865775 8030 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8030 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
68769744 109329 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233187 109329 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
11192346 1993 50 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
68764925 120724 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 120724 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
68767049 120721 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 120721 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
162668957 182178 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182178 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
68769143 109326 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109326 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
11643006 94830 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL256301 94830 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11540494 95026 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257191 95026 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11598 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 666 6 None - 1 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
68767802 109323 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233181 109323 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68764898 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
9430 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL3577945 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
68764898 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 665 1 None - 3 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
11597 667 3 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 667 3 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 667 3 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
46865774 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46886539 8265 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092941 8265 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865774 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1091604 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425294 142833 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389771 142833 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
46865774 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8029 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
66767933 120712 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577933 120712 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
11192943 77271 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77271 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
68772423 171398 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4470701 171398 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
50925394 19132 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19132 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
22143334 187225 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187225 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
68988296 109330 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109330 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11721374 94552 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL254772 94552 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448839 154915 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403889 154915 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448879 155127 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL404904 155127 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
46865775 8030 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8030 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865775 8030 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8030 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
57402219 70664 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 70664 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
68767049 120721 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 120721 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
68867935 109327 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233185 109327 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
11598 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
66768099 120711 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577932 120711 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69035439 77295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
68767124 109322 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233180 109322 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68769143 109326 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109326 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
89845025 109331 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233189 109331 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
44593562 186912 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46865774 8029 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8029 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
68768923 109332 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233190 109332 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
10240064 187844 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 187844 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10129192 187875 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 187875 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
91884571 180878 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 180878 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
10144709 166331 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428602 166331 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425245 85349 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL229316 85349 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44425281 152712 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397749 152712 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11606411 84884 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 84884 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
57335017 69995 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 69995 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10175425 192860 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 192860 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
155531379 171039 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4465351 171039 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44454820 97441 6 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
CHEMBL272369 97441 6 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
44425293 152930 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 152930 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44423283 84883 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 84883 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44593563 192508 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL522688 192508 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44593562 186912 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768865 110634 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263282 110634 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
162666730 181692 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162656188 180333 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180333 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
24794583 180511 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 180511 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44425254 141728 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 141728 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16066354 120722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 120722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
122178128 120719 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 120719 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
42606792 109320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
42606792 109320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL3233178 109320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425250 85625 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230790 85625 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 152995 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 152995 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143255 187275 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187275 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11753466 77287 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77287 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
69035677 77296 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77296 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
155529593 170889 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4463290 170889 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425652 168203 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168203 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
50925394 19132 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19132 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
52941377 19133 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19133 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
68004034 86155 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315922 86155 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
76315270 84476 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
CHEMBL2236474 84476 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
162666730 181692 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389845 172392 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172392 0 None - 1 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11663882 94668 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
CHEMBL255500 94668 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
11713221 95157 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257768 95157 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606147 154804 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL403250 154804 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44448807 154859 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403581 154859 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656715 74856 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 74856 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
70693849 73383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73383 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
49763682 65090 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65090 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44441352 92951 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245686 92951 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44441347 93359 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL247537 93359 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
44425631 141543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 141543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413089 77554 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209411 77554 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11319072 74193 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74193 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11330837 74202 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74202 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11756884 18898 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 18898 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
11562947 89396 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237754 89396 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
57395216 70668 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 70668 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
53322809 58149 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58149 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53321483 58167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
57391766 70673 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 70673 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
162658125 180514 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10184250 73354 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018365 73354 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10186010 73363 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018375 73363 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
46241120 83163 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204258 83163 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
44442557 154386 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401010 154386 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
89823342 125838 0 None - 1 Human 7.0 pIC50 = 7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 125838 0 None - 1 Human 7.0 pIC50 = 7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
56680600 65086 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829607 65086 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44413167 79309 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211560 79309 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
46842232 7800 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7800 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
10161975 93526 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248416 93526 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11843945 77698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209975 77698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
5481702 204109 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 204109 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
56672021 65284 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1833983 65284 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44453208 168855 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL442451 168855 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
11329244 70772 10 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 70772 10 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11272103 123856 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 123856 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
11227368 77290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088383 77290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
25267730 147717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393632 147717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
9885683 18758 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL128640 18758 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823584 125807 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
CHEMBL3650376 125807 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
162658125 180514 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44353196 20725 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL131087 20725 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
10371682 73467 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018541 73467 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
22310939 115165 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL335378 115165 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
70681778 74867 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 74867 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
89823498 125792 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 125792 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
44439169 90343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239170 90343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439169 90343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863202 15043 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210670 15043 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71518728 85981 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314065 85981 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44414578 78000 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL211106 78000 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
11570431 91550 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91550 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353418 22337 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132584 22337 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71768830 110617 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 110617 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57344302 130125 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
CHEMBL3681893 130125 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
72663455 128879 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 128879 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11753664 77269 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088210 77269 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10207639 73464 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018538 73464 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
44595711 136797 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 136797 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
53322810 58164 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58164 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11409228 74185 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74185 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
70689914 74203 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74203 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
44453440 97239 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97239 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
10142792 93308 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93308 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
71768689 110623 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 110623 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
53319664 58369 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58369 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
23630215 62215 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62215 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
53321482 58153 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683064 58153 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53318314 58363 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684692 58363 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53323654 58368 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684699 58368 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
72947191 104781 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 104781 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49763574 65113 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65113 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44442532 93052 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246213 93052 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442594 93340 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247456 93340 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10205937 93529 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248419 93529 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10300282 154239 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400158 154239 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310954 23874 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133839 23874 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71518897 85962 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313782 85962 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442571 154242 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL400160 154242 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11843946 139015 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL379624 139015 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11844079 140945 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL384368 140945 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
23655877 168916 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL443058 168916 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395113 65786 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL183966 65786 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395058 66001 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185032 66001 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
18426192 65675 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL183681 65675 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
44395093 66790 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187476 66790 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
176 394 63 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -3 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44425322 152667 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 152667 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
89823655 125799 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650368 125799 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
44444096 93556 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248617 93556 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44570713 179379 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
CHEMBL474665 179379 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
46830335 8131 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8131 4 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
122181150 121324 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121324 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
49863199 15040 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
CHEMBL1210667 15040 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
44439158 146294 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146294 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
46884818 7789 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7789 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
22310877 19343 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129958 19343 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
42632811 93040 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246104 93040 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127027628 136947 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753826 136947 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44453373 97362 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97362 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44454793 154553 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL401890 154553 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
23656261 88644 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236510 88644 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
53318855 58172 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683083 58172 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
44453409 94995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 94995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44453441 97240 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97240 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
72946982 104750 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 104750 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46842086 7897 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7897 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
44580424 187443 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497576 187443 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11502188 74851 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036752 74851 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10184007 158515 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL409712 158515 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22310971 20286 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130724 20286 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22143196 183405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
56671923 65408 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65408 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54755079 65410 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65410 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
54754968 65411 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65411 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
57400452 70165 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946832 70165 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57393347 69996 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944777 69996 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44416138 138345 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138345 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
9850318 94801 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 94801 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
53324942 58370 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58370 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
12093170 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 180514 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53326225 58362 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684691 58362 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44583283 187702 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 187702 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
22143305 183030 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183030 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
12093170 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 859 27 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 180514 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53324943 58376 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684707 58376 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
57343818 130107 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
CHEMBL3681876 130107 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
86767127 128888 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671260 128888 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
56671924 65416 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834639 65416 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44441358 149314 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL394897 149314 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
52942863 19053 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290186 19053 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44442581 93115 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
CHEMBL246410 93115 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
44442555 93293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247203 93293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44442554 93533 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248423 93533 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11844595 135843 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL373491 135843 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
44353395 19893 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL130403 19893 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
11635092 89395 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237753 89395 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
69212799 77622 2 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77622 2 None - 0 Human 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
56677296 65089 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829611 65089 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25256791 187108 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187108 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
10143025 93104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246397 93104 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444008 154506 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401637 154506 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395194 64436 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL181918 64436 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
25008679 93744 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249607 93744 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
24801178 156300 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL407145 156300 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
44453329 154812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 154812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22310903 22414 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
CHEMBL132662 22414 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
76325121 104762 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115115 104762 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344309 130131 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3681899 130131 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
49863201 15042 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210669 15042 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11663995 146295 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL392494 146295 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11567495 74849 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 74849 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10052388 186969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494541 186969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
22143308 187181 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495717 187181 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44573609 186970 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
CHEMBL494542 186970 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
10256127 73465 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018539 73465 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
44353356 117097 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340072 117097 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
11227383 77294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088387 77294 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71226374 85979 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314061 85979 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
44416066 79377 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
CHEMBL211923 79377 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
22310929 167731 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL434059 167731 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71517402 85955 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313774 85955 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946204 104773 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115267 104773 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44415904 80020 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80020 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11329328 74184 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029411 74184 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425630 85600 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 85600 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44444035 93851 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL250408 93851 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
44353617 19465 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL130065 19465 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
57656942 74689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 74689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
22310953 23761 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133748 23761 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44353170 21215 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131493 21215 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44425650 85703 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 85703 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89853102 110616 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263260 110616 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44415903 80738 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 80738 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
89823502 125793 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650362 125793 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
56643545 130101 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130101 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
11192346 1993 50 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
46947816 65102 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65102 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
56664979 65412 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65412 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671925 65418 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65418 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678508 65470 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65470 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44415899 79664 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 79664 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425641 85639 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 85639 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413258 77405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209063 77405 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425315 85821 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL231252 85821 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425319 85908 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 85908 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53318315 58365 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684695 58365 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
54584109 62218 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62218 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10187492 147257 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147257 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285531 120714 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 120714 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
10152864 187291 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187291 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425288 85588 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230507 85588 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425304 142835 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389773 142835 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53326721 58185 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58185 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
53326901 58374 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684705 58374 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57343820 68612 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
CHEMBL1922816 68612 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
57343819 130104 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL3681873 130104 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
57344311 130133 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681900 130133 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
71719764 85958 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313777 85958 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57396832 69992 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944773 69992 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53320968 58360 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684689 58360 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44442553 93055 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246221 93055 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44442595 165855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427705 165855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44444113 93745 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249608 93745 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11606411 84884 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 84884 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
72946384 104776 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115270 104776 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442583 93117 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246412 93117 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
9890559 65797 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184053 65797 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
11273475 77293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088386 77293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
46884898 7636 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7636 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
22310946 20555 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130937 20555 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
57344310 68594 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922794 68594 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
15518124 137898 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL377432 137898 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
44425649 85702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
54586021 62214 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62214 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
44570779 182986 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480036 182986 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57344299 68614 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL1922818 68614 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
11467577 77289 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088382 77289 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
44453536 97480 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272542 97480 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
22310899 22491 31 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL132725 22491 31 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
89823629 125800 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650369 125800 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
60148505 110622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 110622 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
56643545 130101 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130101 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
86767126 128887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671259 128887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44415880 168773 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 168773 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
57396998 70670 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 70670 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
44425320 85708 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 85708 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453366 157759 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 157759 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
71768794 110615 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263259 110615 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44425286 152713 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397750 152713 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593564 186649 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 186649 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44425258 168341 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438514 168341 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53322299 58366 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684696 58366 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53326226 58378 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684709 58378 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
56675301 65425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834647 65425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44444110 154303 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400483 154303 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844469 77995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL211092 77995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
89823497 125781 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 125781 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
56676473 65477 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834850 65477 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444106 93639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249010 93639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44395144 66658 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186878 66658 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
44593563 192508 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 192508 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46884856 8260 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8260 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
89823512 125833 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650400 125833 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
10414966 154579 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402010 154579 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
89823482 125784 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650353 125784 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
70696469 74864 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036765 74864 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
44425649 85702 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
89823499 125787 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
CHEMBL3650356 125787 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
44413230 138567 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378658 138567 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823444 125805 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 125805 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
44353334 116940 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL339842 116940 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
57343917 130108 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
CHEMBL3681877 130108 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
54769305 86153 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315920 86153 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
68003962 86154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315921 86154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
49764446 65109 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65109 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
54755560 65448 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65448 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44415922 141151 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141151 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
24794624 179036 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179036 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
162657824 180544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4760566 180544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
53326701 58157 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683068 58157 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425633 85614 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 85614 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425648 168139 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168139 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44442590 93339 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93339 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11553489 120708 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577929 120708 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11497533 88759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236722 88759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11541149 145778 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
CHEMBL392097 145778 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
53323664 58383 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684714 58383 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54583187 62245 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62245 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
44425639 85638 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 85638 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
54580190 62242 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62242 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54582215 62231 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62231 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54581190 62233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
162658125 180514 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57344216 130109 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681878 130109 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
71517241 85952 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313771 85952 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025460 136805 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752690 136805 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
10165716 93121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246417 93121 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442559 93298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247208 93298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44442547 154353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400793 154353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
9873546 77683 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209899 77683 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
22310976 116546 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339099 116546 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519050 85965 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313785 85965 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
44395048 65830 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184256 65830 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395062 66365 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185517 66365 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395028 66621 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186689 66621 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395061 66068 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185180 66068 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9825735 93331 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247405 93331 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44444032 93674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249183 93674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844467 77558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
CHEMBL209423 77558 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
44442540 93053 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246218 93053 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
46886537 8264 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092940 8264 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
76321527 104775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115269 104775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
89823389 125819 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650388 125819 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
71518407 85975 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314057 85975 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
10129107 187845 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502248 187845 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44453534 97432 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97432 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
89823621 125798 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 125798 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
22143349 183495 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482387 183495 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44573411 192662 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523857 192662 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
44453620 95092 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257511 95092 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
44573411 192662 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523857 192662 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
70681271 73460 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018533 73460 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
69286635 120718 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 120718 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
162658125 180514 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
72663455 128879 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 128879 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
86767122 128883 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671255 128883 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71519226 85949 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313768 85949 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11647276 74857 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 74857 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83167 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83167 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
56671795 65468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754967 77477 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77477 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
22143241 182668 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 182668 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
44425634 141486 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 141486 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425277 85532 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL230165 85532 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44442592 153149 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398134 153149 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71768688 110611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263255 110611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
71768725 110614 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263258 110614 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44571257 190500 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 190500 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
71745103 125841 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 125841 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
11512375 154131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL399617 154131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10227655 73365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018377 73365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
44415958 80088 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80088 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
44442575 93111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246405 93111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25010616 93717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249413 93717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
25007996 93719 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249415 93719 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844209 80671 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL215515 80671 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
127028590 136905 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753478 136905 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
89823481 125786 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650355 125786 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
89823459 125813 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
CHEMBL3650382 125813 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
89823431 125814 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650383 125814 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
89823495 125820 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650389 125820 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44395256 65138 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL183001 65138 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44593554 188103 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL504065 188103 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
90656019 110620 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263266 110620 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310943 24310 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134230 24310 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10348168 95017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257159 95017 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425317 168292 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168292 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453330 95058 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95058 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
22143225 182983 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480035 182983 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
11620726 90209 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238937 90209 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11620726 90209 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238937 90209 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
127025448 136916 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753563 136916 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
54768835 86166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315933 86166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
11192346 1993 50 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
57656657 74859 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 74859 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 74872 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 74872 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
53322810 58164 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58164 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53326721 58185 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58185 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
10162844 73366 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018378 73366 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
52944966 18850 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 18850 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44425316 141827 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 141827 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53320350 58367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44425646 85673 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 85673 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425653 85802 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 85802 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44353447 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
785 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
CHEMBL337246 3716 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
53326645 58377 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684708 58377 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53324944 58379 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684710 58379 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44425631 141543 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 141543 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89823661 125823 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 125823 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
54583185 62235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62235 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823581 125840 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 125840 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
72663455 128879 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 128879 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71518574 85964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 85964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11632418 74847 1 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 74847 1 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46241720 83147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204242 83147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
135981707 65459 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65459 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44441359 93248 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
CHEMBL246933 93248 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
10206776 154385 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401009 154385 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310896 116948 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339851 116948 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
12093170 859 27 None - 0 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
9431 859 27 None - 0 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
CHEMBL4519152 859 27 None - 0 Human 6.8 pIC50 = 6.8 Binding
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
69315675 73463 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018537 73463 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
44442570 93303 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247214 93303 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
261407 116064 53 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
CHEMBL336399 116064 53 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
44395104 66366 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL185518 66366 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
18426157 123383 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362780 123383 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
57656887 74862 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 74862 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
10239671 187328 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496632 187328 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
44416274 158008 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158008 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46842085 8153 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092294 8153 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
44573450 186940 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL494399 186940 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
46842381 8152 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092293 8152 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
53324139 58151 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683062 58151 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
10346048 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL210606 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44573450 186940 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494399 186940 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
57344217 130110 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
CHEMBL3681879 130110 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
72946775 104756 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 104756 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241717 83154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46240484 83166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83166 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56662695 65474 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65474 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
11669935 58146 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683055 58146 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
44425276 150794 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396101 150794 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
70689909 74187 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029414 74187 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57402219 70664 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 70664 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
53321503 58184 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58184 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54585107 62232 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62232 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
72946205 104763 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115116 104763 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453327 94652 18 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 94652 18 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
70691783 73353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018364 73353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57402124 70179 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947041 70179 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10346048 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL210606 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44441356 96256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL264108 96256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44453327 94652 18 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 94652 18 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44444111 93683 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249209 93683 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656022 110630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263276 110630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
10346048 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL210606 77853 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11670910 88194 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL235657 88194 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71519225 85948 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313767 85948 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763568 65085 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829606 65085 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44444007 93565 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248641 93565 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
11670910 88194 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL235657 88194 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181146 121320 0 None - 0 Mouse 4.8 pIC50 = 4.8 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121320 0 None - 0 Mouse 4.8 pIC50 = 4.8 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44439159 91549 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241501 91549 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863200 15041 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210668 15041 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25268803 151346 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL396571 151346 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL11359 76415 0 None -2 4 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
CHEMBL2068237 76415 0 None -2 4 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
89823461 125796 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 125796 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
44425247 165742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
CHEMBL427110 165742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
52943756 19094 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19094 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425320 85708 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 85708 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
56643545 130101 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130101 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
44573537 192630 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523696 192630 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
44573538 192663 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
CHEMBL523861 192663 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
57392725 67524 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
CHEMBL1910162 67524 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
46885213 8375 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8375 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
68004011 86160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
CHEMBL2315927 86160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
54769752 86180 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316210 86180 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57344296 68609 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL1922813 68609 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
10278257 73361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018373 73361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10207590 73362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018374 73362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
71452241 83155 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83155 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
56657929 65461 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65461 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659197 65473 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65473 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
44425637 85560 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85560 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425317 168292 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168292 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
508869 94996 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 94996 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442587 93376 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93376 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 146667 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 146667 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10278257 73361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
CHEMBL2018373 73361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
53322812 58170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683081 58170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54585109 62244 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62244 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
89823606 125804 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 125804 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
72946982 104750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 104750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344218 68606 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL1922806 68606 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
46241719 83174 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204270 83174 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
46241829 65083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829603 65083 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
10165042 93120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246416 93120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442556 93294 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247204 93294 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
90656026 110633 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263281 110633 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44444001 94076 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251621 94076 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
23441058 65939 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184688 65939 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395160 123291 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL362340 123291 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44415973 80643 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 80643 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425654 85803 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 85803 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44573409 186811 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493575 186811 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
44573409 186811 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493575 186811 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
89823470 125788 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 125788 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
10153373 172027 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL448989 172027 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
86767120 128881 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 128881 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44448915 94629 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255302 94629 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44449054 154652 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402442 154652 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
162666730 181692 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
71768722 110624 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263270 110624 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10239991 187863 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 187863 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10120907 73376 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73376 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
10007642 18917 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 18917 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89844945 109321 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233179 109321 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68767078 120723 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 120723 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
68768752 120725 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
CHEMBL3577947 120725 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
11756884 18898 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 18898 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10007642 18917 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 18917 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
9986630 168234 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL437552 168234 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11627639 94492 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94492 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
57396999 70674 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 70674 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
22143258 183297 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183297 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44593555 188198 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188198 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
70691785 73379 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73379 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
69285794 120716 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 120716 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
122178128 120719 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 120719 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
11555827 146584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
CHEMBL392748 146584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
42606792 109320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
57395218 70666 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 70666 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
44425279 141485 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL387583 141485 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11527661 1990 25 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 1990 25 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 1990 25 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
69285794 120716 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 120716 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68767078 120723 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 120723 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
44583282 172126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172126 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
11597 667 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 667 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 667 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
11421840 77285 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77285 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
50992246 58163 2 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58163 2 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58163 2 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58163 2 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794656 180294 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180294 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
52941377 19133 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19133 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53326386 57865 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1681819 57865 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44573608 186968 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494540 186968 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
54771978 86179 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316209 86179 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
44595711 136797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 136797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
24794624 179036 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179036 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
57400160 130117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681885 130117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
86767125 128886 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671258 128886 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
44449030 94703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255680 94703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44449174 95012 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257143 95012 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44448948 154707 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402749 154707 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
71517242 85953 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313772 85953 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11226430 73391 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018403 73391 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49764322 65110 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65110 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11502371 152594 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 152594 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44425636 85521 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85521 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425629 85599 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230616 85599 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425241 85601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230624 85601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453407 94993 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 94993 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44453442 97241 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97241 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442599 93216 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93216 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285465 120717 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 120717 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11699541 145780 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
CHEMBL392098 145780 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
11605867 166213 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL428378 166213 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54582217 62241 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62241 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
71517576 85942 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313761 85942 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
71518898 85963 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313783 85963 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56675302 65426 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834648 65426 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56669631 65478 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65478 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
25268081 93086 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246313 93086 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
9934977 165802 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL427396 165802 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
44442560 154387 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401011 154387 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11548199 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89492 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
42632863 92924 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245497 92924 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44444104 93637 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249008 93637 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
10957890 22892 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133063 22892 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
44415992 80197 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80197 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453300 96986 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 96986 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44441382 152524 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397595 152524 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11706775 145235 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391668 145235 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11706775 145235 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391668 145235 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453562 155114 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155114 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56678640 65427 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834650 65427 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54768836 86169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315936 86169 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
72947193 104752 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 104752 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10585 1061 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
57401954 68617 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
CHEMBL1922822 68617 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
57656871 74877 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 74877 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
49764447 65091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755801 65429 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65429 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
24801525 97160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97160 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22143104 187475 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 187475 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
44573488 187096 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
CHEMBL495165 187096 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
71517575 85961 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313780 85961 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764700 65107 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829629 65107 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
127025461 136860 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753161 136860 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11692057 144956 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391460 144956 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656585 147098 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL393135 147098 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44444009 93566 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248642 93566 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23441036 66875 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187856 66875 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
24801180 97590 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 97590 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
11577400 58147 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683056 58147 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
71768899 110636 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
CHEMBL3263284 110636 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
44415927 80443 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80443 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11364218 73456 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
CHEMBL2018529 73456 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
24801179 156099 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL406925 156099 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
10458152 77448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209267 77448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
4485 69036 112 None -1 8 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69036 112 None -1 8 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
68003782 86156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315923 86156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
68004010 86159 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315926 86159 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
71530223 85945 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 85945 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764196 65111 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65111 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44573487 192033 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL521697 192033 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
53320171 58168 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58168 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
72948000 104745 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 104745 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774351 130116 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681884 130116 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
46241827 83151 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
CHEMBL2204246 83151 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
10458152 77448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
CHEMBL209267 77448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
44353396 114750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
CHEMBL334766 114750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
10203447 154091 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL399328 154091 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10203447 154091 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL399328 154091 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444103 93602 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248814 93602 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656020 110621 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263267 110621 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310839 21541 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131885 21541 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823443 125822 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650390 125822 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
44395097 66731 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187237 66731 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44442541 154282 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL400382 154282 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44439155 91542 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91542 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53317526 58165 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683076 58165 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
46842235 7754 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7754 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44453298 154700 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 154700 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44570780 183463 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482201 183463 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425649 85702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425305 85637 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
CHEMBL230828 85637 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
69285465 120717 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 120717 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68003997 86173 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315940 86173 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344298 68610 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
CHEMBL1922814 68610 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
71517240 85951 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313770 85951 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56659295 65479 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65479 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425318 149778 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 149778 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44442586 93378 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93378 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442588 93485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248188 93485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801526 97167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
72947413 104777 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 104777 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130118 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681886 130118 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
54755562 65456 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834780 65456 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
25268440 93474 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248153 93474 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44573651 186626 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492376 186626 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
10276594 93531 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248420 93531 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
15290299 22416 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132664 22416 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22310883 116240 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337485 116240 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44573699 187091 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL495151 187091 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44395029 126766 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL365854 126766 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44444002 93562 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248638 93562 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
22310869 19273 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL129833 19273 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
183790 3685 8 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3685 8 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3685 8 None - 2 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
44415939 139603 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 139603 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425638 153000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44415996 79633 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 79633 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
53317527 58173 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683084 58173 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
71518406 85974 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314056 85974 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
89823349 125795 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 125795 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
44593562 186912 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494191 186912 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44453370 155202 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL405632 155202 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
44573538 192663 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523861 192663 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
11606167 90519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239359 90519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11606167 90519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239359 90519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519381 85946 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 85946 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
86767124 128885 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671257 128885 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11489078 73457 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73457 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44447815 154499 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401608 154499 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
53320350 58367 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58367 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
10162782 73358 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73358 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11180885 73387 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018399 73387 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
49763575 65114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65114 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
44444112 154304 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400484 154304 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44449204 95265 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258252 95265 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44395222 66709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187126 66709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10279914 73356 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018368 73356 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
11627639 94492 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL254355 94492 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2010.02.072
44453369 97319 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271726 97319 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
122181144 121318 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121318 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
8447 188362 80 None -12 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -12 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
44415900 79526 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL212542 79526 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
3117 206106 100 None -2 16 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
71517737 85944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313763 85944 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127027956 137055 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
CHEMBL3754764 137055 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
69285531 120714 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 120714 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
57344303 68589 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922789 68589 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344305 68597 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68597 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
46944853 65099 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65099 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
56677288 65112 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65112 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
44416157 80183 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80183 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44413257 77088 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL208685 77088 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11670968 168809 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL442085 168809 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54585108 62234 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62234 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823348 125827 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 125827 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
46241609 83153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
CHEMBL2204248 83153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
25268085 93473 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248151 93473 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10227556 93532 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248421 93532 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
89823555 125779 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650348 125779 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823534 125780 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650349 125780 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823347 125809 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
CHEMBL3650378 125809 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
89834736 125817 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650386 125817 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
53326900 58357 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684682 58357 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
127025447 137009 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754334 137009 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
42632888 93198 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246725 93198 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
57656729 74876 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036779 74876 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44593564 186649 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 186649 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
70688149 74874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 74874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453472 154998 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 154998 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425635 152998 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 152998 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10196988 168898 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 168898 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
44442562 93300 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247210 93300 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44353464 20699 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131065 20699 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
56661559 65419 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834641 65419 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444003 93563 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248639 93563 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44395195 170803 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL446178 170803 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
71517403 85956 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313775 85956 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025728 137011 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
CHEMBL3754349 137011 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
67774360 130106 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL3681875 130106 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
44453563 94646 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255385 94646 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656869 74871 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 74871 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
24801180 97590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 97590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
68004012 86158 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315925 86158 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
72947595 104742 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 104742 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
57656640 74861 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 74861 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
10208946 73370 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018382 73370 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46241718 83158 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83158 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
49763931 65095 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65095 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754723 65422 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65422 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54755081 65446 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65446 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57396901 70180 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947042 70180 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425650 85703 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 85703 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
71768864 110625 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263271 110625 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
10175423 187862 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 187862 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
53325639 58162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53321484 58169 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58169 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44573651 186626 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL492376 186626 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
57344297 68611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
CHEMBL1922815 68611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
46240381 83161 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204256 83161 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
44353223 116010 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL336143 116010 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
46886508 8233 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092739 8233 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
89823438 125810 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
CHEMBL3650379 125810 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
89823624 125811 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
CHEMBL3650380 125811 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
89823464 125831 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650399 125831 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
89823401 125835 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650402 125835 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44425638 153000 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153000 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
72946381 104757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 104757 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
68616341 73385 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73385 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
56678507 65469 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65469 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44416138 138345 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138345 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143196 183405 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183405 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44425642 141814 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 141814 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53325385 58150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683061 58150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53326242 58380 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684711 58380 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54584164 62239 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62239 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44425649 85702 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
183790 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
783 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
10323468 187089 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
CHEMBL495149 187089 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
10119551 93379 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247622 93379 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143196 183405 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183405 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
89823620 125842 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 125842 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44425243 85376 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL229536 85376 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44416041 80022 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80022 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
22310991 19282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129881 19282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395138 123459 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL362889 123459 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
70683355 73468 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018542 73468 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
91754543 125845 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
CHEMBL3650412 125845 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
46241121 83159 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
CHEMBL2204254 83159 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
49863167 15036 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210603 15036 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
46886059 7900 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090561 7900 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025446 136756 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752224 136756 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44439156 91543 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241498 91543 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44415903 80738 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 80738 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
46842084 7833 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7833 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
72946387 104747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 104747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54756038 65447 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65447 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56683044 65471 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65471 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659196 65472 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65472 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
71768830 110617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 110617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
54582216 62236 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62236 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44573486 192555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523054 192555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
11721085 166306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL428559 166306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519055 85971 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314053 85971 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56668306 65386 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834580 65386 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44441396 93150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246522 93150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
57402254 70168 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946835 70168 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44444109 93682 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249208 93682 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44443996 154463 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401387 154463 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
53322813 58174 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683085 58174 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
127028588 136909 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753509 136909 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44415996 79633 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 79633 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
24794656 180294 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180294 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
86767121 128882 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671254 128882 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
162656188 180333 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180333 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44447766 166325 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428594 166325 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
50992246 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1683074 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
25110788 85533 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230166 85533 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425252 141725 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388486 141725 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425255 168318 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168318 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
50992246 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58163 2 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593563 192508 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 192508 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
68769802 120727 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577949 120727 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
11433008 77284 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77284 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44570781 191966 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 191966 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
44425645 85655 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 85655 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53318853 58148 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58148 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
53317041 58381 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684712 58381 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53325460 58186 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58186 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
57395217 70665 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 70665 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
57391767 70675 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 70675 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
53317028 58375 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684706 58375 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
25022597 94895 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 94895 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
66768640 120713 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 120713 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
16066354 120722 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 120722 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
44425644 85654 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 85654 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11353855 74200 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74200 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
70689915 74204 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74204 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
10117480 73368 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73368 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
53325460 58186 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58186 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
22143155 187479 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 187479 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
57656833 74879 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46886538 8234 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092748 8234 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44425653 85802 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 85802 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425272 85608 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230684 85608 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425290 152997 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397997 152997 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53323653 58364 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684694 58364 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
44425644 85654 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 85654 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10281316 73374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
CHEMBL2018386 73374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
10281316 73374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
11353843 74198 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74198 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
24801690 97591 19 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
11527661 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
10218403 187327 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187327 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11527661 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 1990 25 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
70683350 73378 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73378 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
11179439 73388 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73388 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44583280 171883 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 171883 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
44570714 189202 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189202 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143112 187861 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 187861 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
50992246 58163 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58163 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794585 178944 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 178944 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425647 85674 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 85674 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425273 85627 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
CHEMBL230794 85627 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
162666730 181692 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44449031 95254 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL258204 95254 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
10323427 79350 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79350 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
72947411 104778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 104778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11721085 166306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671792 65463 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65463 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
11640044 147715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393631 147715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
44425308 153172 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL398150 153172 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44573486 192555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523054 192555 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
90656025 110632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263280 110632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
76335990 104760 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 104760 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453535 154635 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 154635 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
25033361 153946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 153946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
25033361 153946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 153946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44353367 116800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL339670 116800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
44442542 93332 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247406 93332 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
10409097 66309 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL185282 66309 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
127027624 136863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753178 136863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
10277182 97553 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272860 97553 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22394337 116589 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339275 116589 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
24801690 97591 19 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
46830336 7768 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7768 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11214277 74188 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029415 74188 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
44453268 94686 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255585 94686 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
89823413 125812 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 125812 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
44453474 97422 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97422 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
72946198 104755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 104755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10299408 73352 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018363 73352 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46946058 65101 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829623 65101 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56683121 65480 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65480 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
56676474 65481 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65481 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
53322811 58166 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58166 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54583112 62217 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62217 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46240380 83150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204245 83150 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
57393531 70167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946834 70167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44442596 93039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246098 93039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
73351183 92802 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 92802 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44453477 154764 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL402988 154764 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
44443989 94012 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251217 94012 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
46886507 8000 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1091266 8000 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
89823576 125808 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 125808 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
46842233 7637 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088875 7637 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508741 166908 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL429912 166908 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
90656017 110619 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263264 110619 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
72946198 104755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 104755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946199 104754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 104754 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656854 74878 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 74878 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
46944854 65098 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65098 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54754724 65423 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65423 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44425649 85702 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44413214 77447 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
CHEMBL209263 77447 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
53320349 58361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684690 58361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44570717 183250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183250 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
44425256 85626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230791 85626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
89823552 125782 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 125782 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
76335990 104760 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 104760 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130119 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681887 130119 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
10137967 153414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL398354 153414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10137967 153414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398354 153414 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444099 153874 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL398844 153874 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844329 79630 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL212928 79630 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
23656584 89491 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237966 89491 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44453327 94652 18 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 94652 18 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
42632840 168146 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL436822 168146 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127025730 136798 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752640 136798 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823462 125837 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 125837 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
72947411 104778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 104778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946381 104757 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 104757 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
69285563 120715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 120715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
67774071 130134 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681901 130134 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
54754844 65415 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834638 65415 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
71768831 110627 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263273 110627 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
122181238 121339 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121339 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
23655673 146122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL392366 146122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71518405 85973 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314055 85973 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
23655673 146122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL392366 146122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395169 65826 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL184240 65826 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
11690536 120709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577930 120709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
71519224 85972 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314054 85972 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57400331 70182 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1947044 70182 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
57403811 69998 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944779 69998 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53326703 58171 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683082 58171 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
89823551 125791 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 125791 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
11215504 73454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018527 73454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57398590 69994 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1944775 69994 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
71768862 110629 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263275 110629 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
22310924 19968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130467 19968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22311000 20146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130608 20146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44444006 93604 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248829 93604 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23656432 153867 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
CHEMBL398796 153867 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
44395137 65862 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184390 65862 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
127028587 137031 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754549 137031 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44413328 138728 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378995 138728 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
25270182 92892 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL245290 92892 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
46885159 8290 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8290 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
127027626 136726 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751926 136726 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
44416015 80721 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 80721 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
72947193 104752 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 104752 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656749 74860 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 74860 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
49763571 65087 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65087 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
70687885 74180 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029407 74180 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
71768931 110637 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263285 110637 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44573487 192033 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
CHEMBL521697 192033 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
10141379 73355 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018366 73355 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44425642 141814 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 141814 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
46885029 8165 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8165 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
71518571 85978 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314060 85978 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
71552097 86162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315929 86162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
46240895 83165 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
CHEMBL2204260 83165 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
46927116 65106 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65106 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755919 65428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44612590 136945 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 136945 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
53326702 58160 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683071 58160 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425283 85634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230824 85634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425322 152667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 152667 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44573488 187096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495165 187096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
44442577 93113 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246407 93113 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442578 154590 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402056 154590 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
16720313 84992 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL226376 84992 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
53320967 58359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684684 58359 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
24801344 97282 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL271537 97282 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
44573410 186843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493779 186843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573410 186843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493779 186843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
122181153 121326 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121326 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
122181151 121325 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121325 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
72946387 104747 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 104747 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11553070 74850 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 74850 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46208367 83168 8 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83168 8 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
10195882 70162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946829 70162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44415973 80643 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 80643 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44415939 139603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 139603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44442598 153853 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 153853 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
24801522 160590 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 160590 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
89823526 125826 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 125826 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
57344319 130113 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
CHEMBL3681881 130113 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
9889422 126633 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL365681 126633 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
54755193 65414 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834637 65414 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57395061 69993 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944774 69993 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
71768897 110635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263283 110635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44353197 20570 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130947 20570 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
127025729 136800 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752652 136800 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
127036934 136903 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753474 136903 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
57391797 70166 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946833 70166 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
68004016 86181 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316211 86181 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11342351 77288 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088381 77288 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44415898 80709 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 80709 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
53320970 58373 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684704 58373 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44442566 154240 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL400159 154240 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
22143196 183405 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183405 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44444005 93564 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248640 93564 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
132572938 156248 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156248 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44353377 22968 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133111 22968 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71552260 86171 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315938 86171 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
72946013 104780 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 104780 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
76333441 84475 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
CHEMBL2236473 84475 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
10323427 79350 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79350 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
508877 94618 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 94618 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
53321503 58184 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58184 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
53321615 58372 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684703 58372 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
67772859 123928 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3639807 123928 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10139782 73351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018362 73351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49763569 65088 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829610 65088 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25268436 92996 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245896 92996 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
9885442 20553 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130936 20553 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823586 125803 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 125803 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
72947413 104777 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 104777 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
162666730 181692 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155491018 173511 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
86767123 128884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671256 128884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
11699149 94663 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255478 94663 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
10304021 73372 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73372 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
44415880 168773 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 168773 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44447775 95263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL258246 95263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425643 85615 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 85615 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425271 152708 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397747 152708 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593562 186912 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768755 110612 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
CHEMBL3263256 110612 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
11591956 88907 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236930 88907 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656430 89451 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL237806 89451 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
11548199 89492 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89492 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656431 145804 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
CHEMBL392120 145804 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
44453405 94992 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 94992 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
53318316 58371 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684702 58371 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57395219 70667 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 70667 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
53320973 58382 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684713 58382 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44580590 192866 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 192866 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
24794585 178944 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 178944 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
11283842 73390 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73390 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11273379 74199 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74199 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
54583111 62216 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62216 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
24794583 180511 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 180511 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
53321616 58152 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58152 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
25110716 154667 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 154667 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
44573485 187138 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495368 187138 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573452 187024 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494770 187024 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
68764898 665 1 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 665 1 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 665 1 None - 3 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
10281715 73375 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73375 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
10281715 73375 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73375 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69286635 120718 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 120718 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44571218 183296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57398750 70672 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 70672 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
66768640 120713 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 120713 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
68004002 86157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315924 86157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
67774784 130128 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681896 130128 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
11712754 94623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255266 94623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11555541 154756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402955 154756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11192300 73455 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018528 73455 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11718088 93149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246520 93149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
71519054 85970 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314052 85970 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
10436083 79467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212306 79467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44442565 93108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246401 93108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10299952 154472 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401463 154472 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801343 97324 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
CHEMBL271752 97324 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
44395165 168906 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL442966 168906 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44444098 161115 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
CHEMBL413084 161115 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
44395129 66311 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL185283 66311 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57344313 130135 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130135 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
57344303 130127 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681895 130127 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
71517239 85947 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313766 85947 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946200 104753 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 104753 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946008 104758 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 104758 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
53321483 58167 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58167 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
10279078 73367 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018379 73367 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46240687 83172 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83172 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44447786 94671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 94671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
54584109 62218 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62218 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
69286108 120720 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 120720 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
10218812 192831 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526180 192831 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
89823580 125816 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 125816 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
57344314 68588 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68588 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
76314234 104744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 104744 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72945830 104748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 104748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49764701 65108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829630 65108 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44442543 154283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400383 154283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310945 117558 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340450 117558 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395186 64887 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182598 64887 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
57397013 70169 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1946836 70169 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44395143 66679 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186984 66679 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
24801345 97405 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97405 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
24801345 97405 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97405 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
122181152 121192 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121192 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
5353432 97046 84 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97046 84 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
44573569 192686 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL524030 192686 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
44573569 192686 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL524030 192686 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
44415904 80020 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80020 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425306 141837 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388949 141837 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453408 94994 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 94994 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44593562 186912 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 186912 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
49863225 15046 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210728 15046 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395136 66744 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187284 66744 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9842404 66938 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL188170 66938 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44413147 139183 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL379818 139183 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
25269516 92891 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL245289 92891 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
44439166 90115 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90115 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11237256 73386 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018398 73386 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46945254 65104 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65104 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
89823575 125790 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 125790 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
89823628 125828 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 125828 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
11585168 90257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239143 90257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44442573 93110 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246404 93110 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
44395125 122602 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL361121 122602 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
508727 154780 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403058 154780 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44415945 139019 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL379634 139019 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
127028592 136975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754037 136975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11585168 90257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46241509 83149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83149 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46945857 65100 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829622 65100 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754722 65421 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65421 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
10030247 94964 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256954 94964 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425634 141486 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 141486 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240278 172328 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172328 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
69321774 73462 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018536 73462 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
11844471 79789 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213648 79789 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
71519053 85969 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314051 85969 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11570045 90518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239358 90518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11570045 90518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239358 90518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885028 8337 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8337 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
89823601 125839 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650406 125839 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
70696470 74868 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 74868 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
72946775 104756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 104756 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517401 85954 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313773 85954 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
51039119 175643 29 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 175643 29 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
46241826 83148 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83148 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
56667036 65096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44447789 154683 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402624 154683 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44453472 154998 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 154998 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425640 96481 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96481 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11844470 141204 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL385824 141204 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
11456448 77292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088385 77292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
53321427 58158 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683069 58158 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823598 125844 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 125844 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44395094 66921 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL188075 66921 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
46886057 8314 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8314 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44612589 136907 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753491 136907 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44444000 94075 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251620 94075 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395254 65910 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184582 65910 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
10153431 187745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500786 187745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
11641253 58145 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683054 58145 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
53324140 58154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683065 58154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823656 125834 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 125834 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
53318854 58161 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683072 58161 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
9852285 8176 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092434 8176 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44415942 138152 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL377819 138152 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
53326700 58155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683066 58155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
22143314 192599 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL523403 192599 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
122181236 121337 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121337 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
44593561 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL1187238 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL494580 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
44593561 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12554 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
44415992 80197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
52950180 19154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44442576 93112 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246406 93112 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423285 141634 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL388380 141634 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
89823445 125830 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 125830 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
57344295 130103 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130103 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
23656067 148455 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL394228 148455 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
23656067 148455 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
CHEMBL394228 148455 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
86698131 125785 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650354 125785 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
44439160 168831 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL442254 168831 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439160 168831 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL442254 168831 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25267738 93437 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL247949 93437 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
22311005 19782 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130318 19782 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44415864 80134 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214825 80134 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
10164316 154254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154254 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56683120 65476 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834849 65476 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44449229 94705 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255687 94705 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44453134 97614 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 97614 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
11155781 73461 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
CHEMBL2018534 73461 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
46241610 83157 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83157 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
71519381 85946 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL2313765 85946 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
89823417 125824 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 125824 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44442563 93301 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247211 93301 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344221 68615 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL1922819 68615 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
54772203 86164 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315931 86164 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
54771980 86167 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315934 86167 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
71190126 84477 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
CHEMBL2236475 84477 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
56643545 130101 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130101 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
57344303 130126 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130126 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
11591776 144953 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL391459 144953 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
11185 1960 31 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
25134303 1960 31 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
CHEMBL2178573 1960 31 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
DB16066 1960 31 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
11598084 74854 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 74854 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
10162782 73358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
70691784 73359 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018371 73359 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46241010 83171 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83171 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
49763568 65084 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65084 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
56657930 65462 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65462 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
56683116 65475 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65475 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
89845031 109325 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233183 109325 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
9850318 94801 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 94801 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425646 85673 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 85673 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53317027 58358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684683 58358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44425645 85655 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 85655 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10162782 73358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73358 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11591776 144953 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391459 144953 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
24801690 97591 19 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 97591 19 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
10008367 1991 43 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 1991 43 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 1991 43 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 1991 43 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
24801690 97591 19 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
57656833 74879 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 74879 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
68767109 109324 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
CHEMBL3233182 109324 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
57400451 70163 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946830 70163 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425249 142990 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389888 142990 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11192346 1993 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 1993 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 1993 50 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10165625 73380 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73380 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
44453365 97078 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97078 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
11227168 74201 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74201 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44573650 192607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL523503 192607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
44425648 168139 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168139 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573649 186652 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 186652 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
67011331 74196 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74196 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593563 192508 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 192508 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
53324304 58156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11387511 74192 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74192 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10167417 73377 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73377 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44583281 187652 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 187652 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
44425310 141826 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388868 141826 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11285792 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
801 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
CHEMBL2110727 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
DB11758 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
11285792 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
11285792 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
801 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
CHEMBL2110727 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
DB11758 866 30 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
44573649 186652 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL492569 186652 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
11534473 90268 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
CHEMBL239144 90268 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
71552261 86172 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315939 86172 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11526729 154523 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL401744 154523 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
44448776 154717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402801 154717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656825 74858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 74858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46241608 83156 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83156 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46886482 8175 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092433 8175 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
10482463 95018 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257160 95018 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
183790 3685 8 None -3 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3685 8 None -3 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3685 8 None -3 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
11671120 89450 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
CHEMBL237805 89450 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
22310995 20130 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130598 20130 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
17866152 123521 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL363059 123521 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44395239 65822 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL184220 65822 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
46886056 8313 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1093318 8313 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
11466237 74189 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
CHEMBL2029416 74189 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
52944966 18850 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 18850 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44573609 186970 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494542 186970 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
44593564 186649 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
CHEMBL492564 186649 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
11296618 77291 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088384 77291 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
89823450 125825 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 125825 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
56678497 65387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834581 65387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754845 65420 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834642 65420 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444102 93601 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248813 93601 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
24801690 97591 19 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL273083 97591 19 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2010.02.072
44425321 85709 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 85709 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
11582651 74853 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 74853 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46944855 65103 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65103 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44439170 151389 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396622 151389 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44444107 153947 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399046 153947 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44413311 77430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209171 77430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823456 123892 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3639492 123892 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
11605985 90536 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239569 90536 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11605985 90536 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239569 90536 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44416070 138364 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
CHEMBL378258 138364 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
89823427 125789 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 125789 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
11296325 77268 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088209 77268 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71530223 85945 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 85945 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
53320171 58168 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58168 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54756156 65454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453325 155001 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155001 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
56675300 65424 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834646 65424 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
44442572 93109 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246403 93109 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
24801342 97166 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
CHEMBL270957 97166 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
46240582 83160 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
CHEMBL2204255 83160 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
57403877 70181 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947043 70181 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44353447 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3716 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
52950180 19154 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19154 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89823537 125777 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 125777 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10115566 96961 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL269898 96961 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
56681842 65385 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834579 65385 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
127025159 136826 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752915 136826 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
56661444 65444 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65444 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
23405932 93299 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247209 93299 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
89823506 125815 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 125815 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44573485 187138 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL495368 187138 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
127036603 136987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3754155 136987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
24801346 160702 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL411935 160702 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
508749 66787 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL187469 66787 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
57656701 74881 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036784 74881 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10225909 93527 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248417 93527 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
57344222 130114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
CHEMBL3681882 130114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
44425649 85702 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
68004146 86161 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315928 86161 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
54756045 65457 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65457 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671793 65465 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65465 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44573452 187024 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494770 187024 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
10427222 165188 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL424638 165188 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46886057 8314 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8314 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
72945827 104749 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 104749 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442531 153411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398353 153411 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71519052 85968 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314050 85968 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442584 93118 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246413 93118 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11590644 120710 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577931 120710 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
72948000 104745 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 104745 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46240585 83170 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83170 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44425643 85615 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 85615 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
70697571 77621 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77621 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57398651 70176 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947039 70176 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416273 138412 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL378449 138412 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
90656015 110618 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263262 110618 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44413344 138808 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL379278 138808 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44353369 23040 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL133168 23040 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
44612708 136911 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753526 136911 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344219 130112 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681880 130112 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
71517574 85960 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313779 85960 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57656921 74863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 74863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842383 8261 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8261 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
72946010 104751 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 104751 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517573 85959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313778 85959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57393530 70164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946831 70164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44453372 155203 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155203 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
71768798 110613 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263257 110613 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
9851741 79783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213601 79783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
67774475 130136 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681903 130136 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
44444105 93638 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
CHEMBL249009 93638 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
44413158 79561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
CHEMBL212674 79561 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
89823541 125802 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 125802 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
11699524 94667 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255499 94667 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11605635 95020 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257173 95020 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11534473 90268 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90268 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
54754969 65409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56675205 65464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65464 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44447783 94633 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255312 94633 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
10325032 94672 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255513 94672 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44447782 154774 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
CHEMBL403033 154774 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
10392978 166899 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 166899 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
11421712 74194 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74194 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11365166 74195 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74195 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593564 186649 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 186649 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
22143293 187444 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 187444 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44453368 97318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
22143309 187358 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187358 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
51039119 175643 29 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 175643 29 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
53325639 58162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44580591 187276 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187276 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44425649 85702 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 85702 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
22143293 187444 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 187444 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11700079 149391 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL394955 149391 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10129343 172694 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 172694 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
44425640 96481 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96481 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425309 141825 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 141825 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53324942 58370 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58370 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
60148505 110622 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 110622 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57335017 69995 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 69995 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57391591 69997 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944778 69997 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
162668957 182178 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182178 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
71768900 110626 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263272 110626 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10209478 73373 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73373 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
10300284 73384 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73384 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11752457 74190 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74190 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
69285563 120715 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 120715 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44442561 93106 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246399 93106 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344305 68597 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68597 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
10207591 73070 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2016596 73070 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44571216 172083 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL449674 172083 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
67772854 130115 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
CHEMBL3681883 130115 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
44415957 80642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 80642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
22310876 116424 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL338495 116424 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519381 85946 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 85946 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763804 65094 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65094 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44571258 182669 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479643 182669 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
44439163 89863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238518 89863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44353447 3716 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3716 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3716 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
44453234 97022 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97022 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
127025462 136837 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753005 136837 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
86767119 128880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671252 128880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
76314242 104774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 104774 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44439163 89863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 89863 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46240482 83164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
44447786 94671 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 94671 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
71768721 110631 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263279 110631 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
122178127 120707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL3577928 120707 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
72946202 104761 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115114 104761 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54755083 65413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
44425636 85521 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85521 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 186844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493780 186844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
44453565 168441 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 168441 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
10138789 165956 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427875 165956 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
44573535 186855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
CHEMBL493843 186855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
44573535 186855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493843 186855 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
11563597 91521 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241462 91521 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11563597 91521 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241462 91521 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344315 68599 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
CHEMBL1922799 68599 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
72947595 104742 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 104742 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656713 74855 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 74855 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
11711078 74870 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 74870 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10183362 73357 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018369 73357 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
10392559 154500 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401609 154500 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425637 85560 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85560 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 186844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493780 186844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
24801523 97406 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97406 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22310972 116278 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337720 116278 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395092 126765 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL365853 126765 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
10208555 73364 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018376 73364 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
10208555 73364 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL2018376 73364 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
44395201 66088 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL185190 66088 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
57344313 130135 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130135 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
44415927 80443 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80443 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453473 154999 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404260 154999 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
25008678 93718 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249414 93718 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11570431 91550 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241502 91550 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439173 90276 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
CHEMBL239145 90276 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
52947417 19112 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290522 19112 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
72946199 104754 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 104754 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10206007 73360 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018372 73360 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
11237168 74182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029409 74182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10302973 93119 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246415 93119 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442589 93338 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247439 93338 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423281 141583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL388308 141583 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
44425641 85639 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 85639 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
86698129 125783 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 125783 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
46240481 83173 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
CHEMBL2204269 83173 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
56668313 65460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834784 65460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44353370 23562 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
CHEMBL133569 23562 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
11678573 90208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53324141 58159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683070 58159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11340816 74186 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029413 74186 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10182382 93528 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93528 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11678573 90208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238936 90208 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395055 64173 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64173 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44415995 79642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 79642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
23656260 88643 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236509 88643 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
46842382 8259 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092920 8259 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508744 65883 1 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL184474 65883 1 None - 0 Human 4.2 pIC50 = 4.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
127025160 136900 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753428 136900 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344316 68592 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922792 68592 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344230 130120 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
CHEMBL3681888 130120 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
11080 28872 74 None -1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28872 74 None -1 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
9851741 79783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213601 79783 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425654 85803 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 85803 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53321484 58169 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58169 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44442580 93114 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
CHEMBL246409 93114 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
44413310 138430 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378517 138430 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
72948004 104779 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 104779 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656719 74866 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 74866 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
54580189 62240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782575 62240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
23656433 88335 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236269 88335 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
72945830 104748 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 104748 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67220645 74880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 74880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
127027955 136729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
CHEMBL3751958 136729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
44415898 80709 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 80709 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
11478362 73459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018532 73459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44453592 159508 20 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 159508 20 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44442582 93116 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
CHEMBL246411 93116 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
9952114 123865 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL363908 123865 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
71518408 85976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314058 85976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
54772206 86163 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315930 86163 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
54772204 86165 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315932 86165 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
54772205 86168 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315935 86168 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
72663455 128879 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 128879 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11599317 95116 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL257628 95116 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
53324304 58156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
10228435 73369 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018381 73369 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46927117 65097 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65097 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56661451 65467 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65467 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44573699 187091 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495151 187091 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11306757 73389 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73389 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57391765 70671 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 70671 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
44425244 151272 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396517 151272 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
23630215 62215 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62215 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10120067 73381 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73381 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
52943756 19094 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19094 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425274 150325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL395721 150325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
24801690 97591 19 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 97591 19 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44425647 85674 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 85674 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423282 84850 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL226017 84850 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
162648673 179370 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4746510 179370 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425633 85614 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 85614 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44570718 183251 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183251 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11621035 154130 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
CHEMBL399616 154130 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
10052388 186969 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
CHEMBL494541 186969 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
57391768 70669 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 70669 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
44573608 186968 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 186968 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11180383 77270 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77270 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143294 192823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 192823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
49763686 65093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
508750 167970 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 167970 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
127028586 136982 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754119 136982 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
11844468 139066 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL379742 139066 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
44395088 66835 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187701 66835 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10209102 93105 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246398 93105 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344320 130121 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681889 130121 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
72948001 104743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 104743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241611 83152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204247 83152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
57344232 130122 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681890 130122 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
44395126 65082 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182958 65082 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395126 65082 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL182958 65082 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
57656915 74869 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036772 74869 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
11341950 73458 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018531 73458 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
42632836 92954 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245696 92954 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
68004094 86174 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315941 86174 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57396900 70178 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947040 70178 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416041 80022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
44416015 80721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 80721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44413144 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL378784 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44413144 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL378784 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
23656434 89188 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237538 89188 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44442569 93302 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247213 93302 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44415958 80088 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80088 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
11563451 151386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396621 151386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453533 97431 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272330 97431 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10008367 1991 43 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 1991 43 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 1991 43 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 1991 43 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
11563451 151386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44425321 85709 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 85709 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44425651 142645 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 142645 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
56643545 130102 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681871 130102 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10025168 66652 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186855 66652 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
10025168 66652 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186855 66652 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
44395036 124532 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL364405 124532 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
127027625 136730 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751959 136730 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
22143293 187444 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 187444 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57343816 130105 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681874 130105 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
53320974 58384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684715 58384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57344314 68588 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68588 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44442564 93107 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246400 93107 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
46842236 7785 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089849 7785 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413411 77385 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL209002 77385 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
44453507 168412 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168412 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
69286108 120720 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 120720 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
71518574 85964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 85964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
89823496 125794 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 125794 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
89823439 125778 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 125778 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44573568 186887 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL494019 186887 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
44439164 90342 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239169 90342 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439164 90342 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239169 90342 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44573650 192607 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523503 192607 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
10323468 187089 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
CHEMBL495149 187089 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
72948001 104743 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 104743 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44573568 186887 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494019 186887 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
72947593 104759 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 104759 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44413144 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL378784 138689 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44442544 93333 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247407 93333 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44353190 116066 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL336421 116066 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
46240785 83169 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83169 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
72947593 104759 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 104759 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
70692344 74848 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 74848 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
11844083 77639 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
CHEMBL209696 77639 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
44395238 123327 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362536 123327 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
42632830 92953 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245694 92953 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44416156 80740 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL215768 80740 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
24801345 97405 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97405 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
44453171 95293 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95293 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10300705 97449 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
CHEMBL272407 97449 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
53325639 58162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
57402059 69999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 69999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425319 85908 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 85908 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
46241011 83162 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204257 83162 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
44444114 93775 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
CHEMBL249811 93775 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
24801180 97590 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 97590 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
122181145 121319 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121319 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44395232 66663 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186913 66663 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
71518727 85980 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314064 85980 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
57656808 74873 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036776 74873 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
54768838 86170 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315937 86170 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344295 130103 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130103 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
57344303 130126 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130126 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44425635 152998 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 152998 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413076 139618 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL380258 139618 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425652 168203 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168203 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10312346 187878 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 187878 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
50991056 62237 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62237 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10218843 172217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425651 142645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 142645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53319664 58369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
53322810 58164 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58164 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593561 12554 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12554 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12554 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
71768689 110623 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 110623 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22143346 172082 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172082 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
54580188 62238 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62238 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
11606702 145221 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391662 145221 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44449175 95062 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257351 95062 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
49763685 65092 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829614 65092 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44612590 136945 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 136945 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44415899 79664 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 79664 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
11844212 98196 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL277279 98196 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44415995 79642 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 79642 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
25007995 154332 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400680 154332 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844212 98196 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL277279 98196 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
11662833 88758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236721 88758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181235 121336 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121336 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
44416125 80509 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215333 80509 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
57344300 130123 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
CHEMBL3681891 130123 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
71517577 85943 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313762 85943 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
76314234 104744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 104744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44425318 149778 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 149778 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
90656021 110628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263274 110628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
89823460 125818 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650387 125818 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
72946200 104753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 104753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
56668309 65445 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65445 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
127028591 136929 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3753683 136929 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823691 125797 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650366 125797 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
11843812 79494 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212423 79494 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
57344307 130129 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681897 130129 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
89823344 125829 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 125829 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
11843812 79494 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
CHEMBL212423 79494 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
89823453 125836 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
CHEMBL3650403 125836 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
508729 95091 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95091 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
46884855 8219 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8219 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413399 79119 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211404 79119 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
70687886 74181 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
CHEMBL2029408 74181 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
44573451 186984 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494591 186984 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
25008849 93746 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249609 93746 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
46945255 65105 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829627 65105 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
44573451 186984 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494591 186984 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
11690139 74875 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 74875 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415957 80642 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 80642 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
70683619 74179 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029406 74179 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22310850 116307 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337857 116307 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44413137 78482 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
CHEMBL211292 78482 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
72947191 104781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 104781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774197 130130 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681898 130130 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
72946013 104780 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 104780 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10207542 73371 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018383 73371 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
24801524 166774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL429425 166774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22268768 154382 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
CHEMBL400968 154382 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
44395066 123944 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL363994 123944 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
71518570 85977 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314059 85977 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
72948004 104779 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 104779 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71716742 85957 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313776 85957 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44453471 97421 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97421 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10228205 93295 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247205 93295 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344303 130126 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130126 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57402059 69999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 69999 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
25268795 147975 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393835 147975 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
86767120 128881 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 128881 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44449081 95069 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257385 95069 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11634928 168325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL438353 168325 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606702 145221 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145221 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671794 65466 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65466 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44595711 136797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 136797 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44416157 80183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425630 85600 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 85600 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11330529 74191 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74191 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
24801689 97345 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97345 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425242 85616 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230727 85616 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
54583186 62243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10232019 73382 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73382 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
53322811 58166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54586021 62214 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62214 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
10008367 1991 43 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 1991 43 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 1991 43 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 1991 43 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
10281715 73375 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73375 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
22143146 183324 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183324 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
76314242 104774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 104774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11633080 93199 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
CHEMBL246728 93199 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
44442591 93380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247635 93380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310914 24124 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134072 24124 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10459336 73466 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018540 73466 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
44442574 154589 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402055 154589 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11634118 58144 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683053 58144 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
89823507 125801 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 125801 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
56678506 65458 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834782 65458 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57401421 67523 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
CHEMBL1910161 67523 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
127025445 136937 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753719 136937 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
72663455 128879 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 128879 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44416274 158008 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158008 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425639 85638 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 85638 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11843813 141369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL386865 141369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
44395079 66662 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186899 66662 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44439157 91248 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
CHEMBL240853 91248 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
49863168 15037 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
CHEMBL1210604 15037 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
71519227 85950 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313769 85950 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11318368 74183 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
CHEMBL2029410 74183 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
89823428 125806 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 125806 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
72945827 104749 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 104749 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57391487 130137 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681904 130137 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44444100 93600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248812 93600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44425316 141827 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 141827 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
25268442 93516 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL248358 93516 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
508870 97027 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270205 97027 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
22310992 22906 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL133075 22906 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
57344301 130124 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
CHEMBL3681892 130124 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
508742 95132 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95132 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
44453538 97481 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97481 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
72946008 104758 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 104758 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10278862 93296 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247206 93296 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22143200 187182 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187182 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
9956260 157141 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL408172 157141 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
127025444 136744 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752110 136744 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
57656938 74865 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 74865 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44415922 141151 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141151 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
57344318 68591 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922791 68591 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344317 68590 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922790 68590 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
72946010 104751 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 104751 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11510932 74852 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 74852 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
46886061 7901 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090562 7901 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44442558 93297 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247207 93297 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22310965 19392 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130008 19392 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46885027 8336 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8336 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
11180808 2512 47 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2512 47 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2512 47 None - 1 Human 9.3 pKd = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
155491018 173511 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 171932 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 171932 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155491018 173511 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173511 1 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 171932 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 171932 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11180808 2512 47 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2512 47 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2512 47 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
71717723 87401 0 None 51 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
CHEMBL2338392 87401 0 None 51 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
155554273 173641 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 173641 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
155554273 173641 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 173641 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 181692 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162666730 181692 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155554106 174896 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 174896 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 174657 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 174657 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 174657 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 174657 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155554106 174896 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 174896 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
71718331 87400 0 None 208 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
CHEMBL2338391 87400 0 None 208 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
71719547 87402 0 None 50 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
CHEMBL2338393 87402 0 None 50 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
118734584 118191 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417124 118191 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
53389845 172392 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172392 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389845 172392 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172392 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 174709 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 174709 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 174709 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 174709 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10585 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169159 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169159 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
118734578 118184 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417117 118184 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
10585 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169159 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169159 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389660 170917 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 170917 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389660 170917 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 170917 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
155553917 173631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 173631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155553917 173631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 173631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389637 170000 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170000 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389637 170000 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170000 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 181692 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
15985912 83561 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83561 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461438 83562 0 None 100 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 83562 0 None 100 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83564 0 None 14 2 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83564 0 None 14 2 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450658 83578 0 None 15 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 83578 0 None 15 3 Human 8.0 pKi = 8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83561 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83561 0 None 2 3 Human 8.0 pKi = 8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
118734680 118199 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417225 118199 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734682 118201 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417227 118201 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
12093167 171759 30 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 171759 30 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823581 125840 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 125840 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10436045 3460 3 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 7.0 pKi = 7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
71461439 83567 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 83567 0 None 10 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452487 83568 0 None 12 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 83568 0 None 12 3 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
71454247 83570 0 None 15 2 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207090 83570 0 None 15 2 Human 7.0 pKi = 7 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
155539148 172235 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172235 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155539148 172235 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172235 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823497 125781 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 125781 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
155536512 171639 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 171639 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
3013430 20931 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
183790 3685 8 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.0 pKi = 7.0 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155536512 171639 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 171639 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
89823576 125808 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 125808 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
89823413 125812 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 125812 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
118734676 118196 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417221 118196 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
12093167 171759 30 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 171759 30 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823461 125796 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 125796 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
118734684 118203 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417229 118203 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
71745103 125841 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 125841 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3685 8 None -3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
71454248 83581 0 None 25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 83581 0 None 25 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
71214976 83582 0 None 79 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 83582 0 None 79 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
155545321 172882 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 172882 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823621 125798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 125798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
71463165 83566 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207086 83566 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
9870980 154110 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL399472 154110 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
25110660 154333 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154333 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
10436045 3460 3 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734580 118187 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417120 118187 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734582 118189 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417122 118189 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
118734688 118207 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417233 118207 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
155545321 172882 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 172882 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823598 125844 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 125844 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3685 8 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734694 118214 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417240 118214 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
9902578 170789 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 170789 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118723411 115824 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359300 115824 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
155523645 170311 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170311 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155523645 170311 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170311 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
9902578 170789 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 170789 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3685 8 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
54597147 160825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
CHEMBL4126162 160825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
118734571 118177 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417110 118177 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
118734575 118181 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417114 118181 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
155521447 170017 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170017 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
89823526 125826 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 125826 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
155521447 170017 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170017 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155518928 169777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 169777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
155518928 169777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 169777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
71214710 83565 0 None 39 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 83565 0 None 39 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10293022 170532 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 170532 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
3013430 20931 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155530253 170955 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 170955 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
155545804 172925 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 172925 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 174566 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 174566 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155545804 172925 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 172925 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 174566 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 174566 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155535265 171453 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 171453 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155530253 170955 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 170955 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
71456007 83572 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 83572 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
89823445 125830 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 125830 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
10436045 3460 3 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
53389980 171661 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 171661 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155535265 171453 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 171453 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
5353432 97046 84 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97046 84 None -1 3 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
9924108 171207 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171207 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
10436045 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10293022 170532 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 170532 12 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823661 125823 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 125823 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
53389980 171661 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 171661 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3685 8 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22335694 170992 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 170992 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9924108 171207 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171207 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
781 3344 71 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
155522874 170272 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170272 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155522874 170272 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170272 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
22335694 170992 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 170992 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9902204 169559 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 169559 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3685 8 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
44353447 3716 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9902204 169559 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 169559 12 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
162671727 182389 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182389 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
118734693 118213 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417239 118213 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823498 125792 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 125792 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
3794409 170189 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170189 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
76167595 160917 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127538 160917 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
118734686 118205 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417231 118205 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
118734691 118211 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417237 118211 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
183790 3685 8 None -3 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3685 8 None -3 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3685 8 None -3 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
71718930 87399 0 None 75 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
CHEMBL2338390 87399 0 None 75 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
155551912 174564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 174564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155551912 174564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 174564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155540798 172366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734572 118178 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417111 118178 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
155540798 172366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172366 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389710 171715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 171715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
71576618 118185 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417118 118185 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
53389710 171715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 171715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
73334813 118209 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417235 118209 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
162666730 181692 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155560784 174479 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 174479 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
155560784 174479 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 174479 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
183790 3685 8 None -3 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 8.6 pKi = 8.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155541801 172487 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 172487 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155527193 170603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 170603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155527193 170603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 170603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
3013430 20931 1 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
3794409 170189 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170189 7 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
89823496 125794 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 125794 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
781 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3460 3 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 5.7 pKi = 5.7 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734576 118182 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417115 118182 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
89823628 125828 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 125828 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
183790 3685 8 None -3 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155550777 173715 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 173715 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
3796276 170283 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170283 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 170563 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 170563 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 172754 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 172754 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
3796276 170283 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170283 7 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 170563 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 170563 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 172754 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 172754 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
781 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162671727 182389 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182389 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155550777 173715 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 173715 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155513605 169213 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169213 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155513605 169213 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169213 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155553131 173539 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 173539 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3460 3 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
3013430 20931 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734581 118188 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417121 118188 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
118734683 118202 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417228 118202 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
3013430 20931 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
9967465 171521 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 171521 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967465 171521 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 171521 11 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
68070944 160913 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127496 160913 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
118734690 118210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417236 118210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
71450657 83574 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 83574 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
15604497 83579 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 83579 0 None 39 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
44309012 102350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
71463166 83576 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207096 83576 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
44309012 102350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102350 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3344 71 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44353447 3716 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
3013430 20931 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
11080 28872 74 None -1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28872 74 None -1 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
155553131 173539 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 173539 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
89823470 125788 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 125788 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
12093163 173830 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 173830 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
12093163 173830 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 173830 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3685 8 None -3 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723406 115822 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359295 115822 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
89823507 125801 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 125801 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
89823552 125782 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 125782 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
183790 3685 8 None -3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
3013430 20931 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
44353447 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
155540563 171970 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 171970 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9949615 137676 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
CHEMBL376981 137676 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
89823551 125791 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 125791 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
118734685 118204 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417230 118204 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
155541801 172487 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 172487 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 171479 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 171479 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
53389636 171834 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 171834 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155543260 172718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 172718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 171479 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 171479 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155543260 172718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 172718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389636 171834 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 171834 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 181692 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 180514 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175380 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175380 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
86698129 125783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 125783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 20931 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155540563 171970 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 171970 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823349 125795 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 125795 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
118734573 118179 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417112 118179 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
162671079 182270 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182270 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
89823575 125790 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 125790 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
15985914 83560 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83560 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461440 83577 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 83577 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
162671079 182270 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182270 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155513751 169234 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169234 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
25110660 94355 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL253424 94355 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
44353447 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
44353447 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
155513751 169234 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169234 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
89823537 125777 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 125777 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823606 125804 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 125804 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
89823656 125834 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 125834 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44353447 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9967349 172496 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 172496 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967349 172496 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 172496 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823580 125816 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 125816 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
118734678 118197 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417223 118197 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
71214725 83563 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 83563 0 None 15 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10257042 202658 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 202658 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
162666730 181692 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 181692 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175380 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175380 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155520385 169882 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 169882 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155520385 169882 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 169882 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
183790 3685 8 None -3 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 8.4 pKi = 8.4 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734579 118186 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417119 118186 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
162658125 180514 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
118734687 118206 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417232 118206 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
118734574 118180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417113 118180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
118734692 118212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417238 118212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734577 118183 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417116 118183 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
10257042 202658 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 202658 0 None 12 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
11632418 74847 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 74847 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
118734681 118200 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417226 118200 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
176 394 63 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -3 31 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
89823586 125803 0 None - 1 Human 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 125803 0 None - 1 Human 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
781 3344 71 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
89823444 125805 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 125805 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
3013430 20931 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734671 118194 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417216 118194 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
89823344 125829 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 125829 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
155534565 171405 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171405 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155529754 170895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 170895 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10111333 174894 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 174894 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155529754 170895 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 170895 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155534565 171405 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171405 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44573568 186887 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL494019 186887 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
782 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
CHEMBL432713 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
10436045 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
71457815 83571 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 83571 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
71452488 83573 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 83573 0 None 19 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
10436045 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3460 3 None -85 13 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
15985981 83559 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
CHEMBL2207079 83559 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
71454246 83569 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 83569 0 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
155522058 170077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155522058 170077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
781 3344 71 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
118734675 118195 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417220 118195 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823462 125837 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 125837 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
10436045 3460 3 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
22335665 172895 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 172895 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22335665 172895 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 172895 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
781 3344 71 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
3013430 20931 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823427 125789 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 125789 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
162658125 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10111333 174894 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 174894 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823620 125842 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 125842 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
162658125 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 180514 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
155531561 171084 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171084 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155531561 171084 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171084 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3685 8 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
89823439 125778 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 125778 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
71456008 83575 0 None 25 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 83575 0 None 25 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
162672927 182601 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 182601 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44309012 102350 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102350 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
44309012 102350 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102350 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3344 71 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9870980 202582 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71297 202582 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
9967166 169406 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169406 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
118723408 115823 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359297 115823 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
9967166 169406 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169406 11 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155559153 174209 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174209 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
89823506 125815 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 125815 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
155559153 174209 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174209 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
44353447 3716 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823342 125838 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 125838 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 20931 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155553573 173605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 173605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155553573 173605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 173605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734583 118190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417123 118190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL11359 76415 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
CHEMBL2068237 76415 0 None -2 4 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
44353447 3716 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
10436045 3460 3 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3460 3 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3460 3 None -85 13 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118723021 115767 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3358698 115767 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
118734679 118198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
CHEMBL3417224 118198 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
3013430 20931 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 20931 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823417 125824 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 125824 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44353447 3716 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3716 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3716 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823348 125827 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 125827 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
25110660 154333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
9857981 170220 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170220 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
25110660 154333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154333 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
89823541 125802 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 125802 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
89823450 125825 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 125825 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
22725647 173127 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173127 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9857981 170220 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170220 11 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118734689 118208 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417234 118208 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
89823428 125806 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 125806 0 None - 1 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
4485 69036 112 None -1 8 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69036 112 None -1 8 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
781 3344 71 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3344 71 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3344 71 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162672927 182601 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 182601 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
22725647 173127 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173127 0 None 3 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3685 8 None -3 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3685 8 None -3 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3685 8 None -3 2 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723412 115825 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359301 115825 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
10133557 171972 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 171972 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10133557 171972 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 171972 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
8447 188362 80 None -12 13 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -12 13 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
9945265 170617 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 170617 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
3117 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
9945265 170617 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 170617 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
46208367 83168 8 None - 1 Mouse 5.0 pKi = 5.0 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83168 8 None - 1 Mouse 5.0 pKi = 5.0 Binding
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
12093170 859 27 None - 0 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
9431 859 27 None - 0 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
CHEMBL4519152 859 27 None - 0 Human 5.3 pIC50 < 5.3 Binding
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
4410 3088 99 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3088 99 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3088 99 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3088 99 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3088 99 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
11598 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
23725177 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
CHEMBL4442783 666 6 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
10586 2108 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
11617815 2108 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
46198579 3013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
9979 3013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
DB14955 3013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
176 394 63 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3117 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4485 69036 112 None -1 8 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
CHEMBL193 69036 112 None -1 8 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
10585 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
145996522 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
CHEMBL4531005 1061 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
11560568 1855 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
3502 1855 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
CHEMBL1082152 1855 0 None - 1 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
44353447 3716 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
785 3716 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
CHEMBL337246 3716 0 None - 1 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
781 3344 71 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
9953769 3344 71 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
CHEMBL134074 3344 71 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
10436045 3460 3 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
782 3460 3 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
CHEMBL432713 3460 3 None -85 13 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
183790 3685 8 None -3 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3685 8 None -3 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3685 8 None -3 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
183790 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
183790 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
783 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
CHEMBL1178786 3685 8 None -3 2 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060