Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
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
164609465 183897 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells by luciferase reporter gene assayAgonist activity at frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells by luciferase reporter gene assay
ChEMBL 1425 27 21 24 -9.2 CSCC[C@@H]1NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)O)NC1=O nan
CHEMBL4847020 183897 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells by luciferase reporter gene assayAgonist activity at frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells by luciferase reporter gene assay
ChEMBL 1425 27 21 24 -9.2 CSCC[C@@H]1NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)O)NC1=O nan
164610002 184065 0 None -58 4 Human 9.0 pIC50 = 9 Functional
Antagonist activity at Wnt3a-stimulated frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1427 49 23 24 -9.7 CSCC[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O nan
CHEMBL4849630 184065 0 None -58 4 Human 9.0 pIC50 = 9 Functional
Antagonist activity at Wnt3a-stimulated frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated frizzled-1 (unknown origin) expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1427 49 23 24 -9.7 CSCC[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O nan
10197 3909 0 None 1 5 Human 9.2 pIC50 ~ 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22753465




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
164610002 184065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1427 49 23 24 -9.7 CSCC[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O nan
CHEMBL4849630 184065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1427 49 23 24 -9.7 CSCC[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(N)=O nan
164615482 183967 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1565 50 24 23 -7.1 CC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O)[C@@H](C)O nan
CHEMBL4848198 183967 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 1565 50 24 23 -7.1 CC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O)[C@@H](C)O nan
164611733 184259 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 2566 84 43 36 -12.7 CC[C@H](C)[C@H](NC(=O)CNC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)C(C)C)[C@@H](C)O nan
CHEMBL4852279 184259 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assayAntagonist activity at Wnt3a-stimulated rat frizzled-1 expressed in human HEK293superTOP flash cells incubated for 24 hrs by luciferase reporter gene assay
ChEMBL 2566 84 43 36 -12.7 CC[C@H](C)[C@H](NC(=O)CNC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)C(C)C)[C@@H](C)O nan
155554358 174044 0 None -8 2 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3291 99 40 42 -1.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1cccc(Cl)c1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(C)=O)[C@H](C)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cccc(Cl)c1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(C)=O)[C@H](C)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500
CHEMBL4557583 174044 0 None -8 2 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3291 99 40 42 -1.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1cccc(Cl)c1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(C)=O)[C@H](C)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cccc(Cl)c1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(C)=O)[C@H](C)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500
155517545 169633 0 None -3 2 Human 9.0 pKd = 9.0 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3167 97 40 42 -4.7 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(C)=O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500
CHEMBL4445160 169633 0 None -3 2 Human 9.0 pKd = 9.0 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3167 97 40 42 -4.7 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(C)=O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500
155556372 173908 0 None -2 2 Human 8.6 pKd = 8.6 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3588 107 42 46 -3.7 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(C)=O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500
CHEMBL4554351 173908 0 None -2 2 Human 8.6 pKd = 8.6 Binding
Binding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assayBinding affinity to recombinant human Frizzled-1 (Gln73 to His253 residues)/human IgG1 chimeric protein expressed in mouse NS0 cells by SPR assay
ChEMBL 3588 107 42 46 -3.7 CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(C)=O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.9b00500