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
CHEMBL218994 207658 0 None 1 2 Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165734 206785 0 None - 1 Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163460 206776 0 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163463 206777 6 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 210690 1 None - 1 Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163467 206778 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165797 206792 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165767 206788 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44189349 181213 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181213 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL577772 214000 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 214000 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1165735 206786 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL504097 212403 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163473 206780 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
162650062 179510 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4748168 179510 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL437430 211970 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1016/j.bmc.2009.07.058
145965592 163864 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163864 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973990 164133 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL524855 213846 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL510618 213809 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162646037 178934 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 178934 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL1165796 206791 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL1165793 206789 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm901294u
CHEMBL1165794 206790 1 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL2372899 208559 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL385616 210611 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(=O)O 10.1021/jm0111043
CHEMBL53181 213931 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372897 208558 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
145967082 163549 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162663320 181435 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780734 181435 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
162648628 179275 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179275 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593663 214037 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
162644923 178849 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 178849 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
145978068 163184 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163184 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164177 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164177 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL406590 210868 0 None - 1 Human 6.0 pEC50 = 6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL505358 212421 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162655718 180115 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4755542 180115 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24953411 13969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197619 13969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL578654 13969 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
162668637 182065 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182065 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
24952710 13954 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197510 13954 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574732 13954 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953059 13951 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197507 13951 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574726 13951 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
162660425 180716 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762329 180716 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163438 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
2151 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
9797568 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
CHEMBL192359 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
15983447 85220 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228413 85220 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
15983564 85239 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228525 85239 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
10407901 10743 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172234 10743 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799325 14268 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173106 14268 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200251 14268 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
145967082 163549 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163438 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
46897997 14251 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172407 14251 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200175 14251 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
145965592 163864 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163864 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607810 214056 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163134 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24954831 13949 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197503 13949 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574527 13949 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163438 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163438 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145965592 163864 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163864 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953055 13938 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197455 13938 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572883 13938 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
11983241 85228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228470 85228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL607811 214057 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163134 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372905 208565 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
11325792 139637 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
CHEMBL380346 139637 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
15983822 85419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229713 85419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162666444 181690 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783832 181690 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
49799029 14271 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173147 14271 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200258 14271 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983820 161198 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL413787 161198 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
162664787 181632 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783104 181632 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209317 5 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44409467 74406 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL203080 74406 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572699 74406 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799289 14281 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1173399 14281 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200283 14281 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
145966260 163834 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163834 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372904 208564 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977223 163438 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162671682 182307 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182307 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
15983443 136810 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL375275 136810 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
15983686 137558 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376582 137558 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
162649626 179487 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4747883 179487 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163438 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608099 214060 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
15983445 85219 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228412 85219 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145973990 164133 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49798987 14255 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172604 14255 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200193 14255 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
15983693 168827 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL442230 168827 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162669582 182147 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789784 182147 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
145973104 164177 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164177 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11524599 76374 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL206596 76374 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145978068 163184 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163184 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372903 208563 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799280 14275 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173239 14275 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200268 14275 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
24954830 13932 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197440 13932 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572398 13932 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
15983690 85489 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229924 85489 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163471 206779 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL298803 209159 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm0111043
CHEMBL427632 211610 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL408106 210954 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL426020 211595 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2372896 208557 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145967082 163549 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608098 214059 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
162662463 181451 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780893 181451 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
24795079 13939 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197471 13939 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573392 13939 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
46897998 14240 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1172180 14240 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1200148 14240 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
46897996 14249 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1172224 14249 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1200156 14249 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
15983570 85445 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229868 85445 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
162670598 182340 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182340 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL2372895 208556 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799327 14272 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173170 14272 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200259 14272 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162677235 182913 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 182913 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
9797568 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL192359 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL1163477 206782 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46897995 14248 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1172223 14248 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200155 14248 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
145966260 163834 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163834 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24955192 13948 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197496 13948 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574305 13948 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
145977223 163438 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799291 14282 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173400 14282 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200284 14282 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162653594 179956 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4753729 179956 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
49799368 14260 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172764 14260 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200219 14260 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983449 85227 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228461 85227 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
10213684 3872 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
2152 3872 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL414256 3872 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372907 208566 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163134 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372902 208562 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)CCC(=O)O)C(=O)O 10.1021/jm0111043
CHEMBL1627325 207068 0 None -102 8 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
162657061 180318 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180318 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL216349 207581 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1)C(=O)O 10.1021/jm0111043
CHEMBL3104471 209317 5 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
10996495 179332 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL4746051 179332 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL385962 210623 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162649156 179248 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745061 179248 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
9797568 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
CHEMBL192359 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
24952707 13930 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197438 13930 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572391 13930 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983691 85393 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229659 85393 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163475 206781 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
145973104 164177 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164177 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
45481596 13963 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197565 13963 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL576746 13963 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
11696838 76803 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL207823 76803 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573857 76803 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 163834 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163834 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 180711 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 180711 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162644289 181209 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777923 181209 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
145973990 164133 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953056 13958 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197533 13958 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575629 13958 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
145965592 163864 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163864 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953060 13933 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197441 13933 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572423 13933 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163438 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977587 163134 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145967082 163549 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145978068 163184 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163184 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24952352 13944 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197480 13944 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573575 13944 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1163479 206783 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
15983818 85418 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229710 85418 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164133 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983826 85420 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229714 85420 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
24953414 13946 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197484 13946 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573836 13946 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799486 14288 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173689 14288 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200298 14288 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983560 85229 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228471 85229 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL593662 214036 9 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900604g
162651887 179691 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 179691 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162645261 179105 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4743591 179105 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
10474282 68770 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL192389 68770 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
49798794 14219 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1170888 14219 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200021 14219 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983562 85230 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228472 85230 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
16126405 136654 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL374817 136654 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
24953410 13934 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197442 13934 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572439 13934 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
24952350 13979 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197698 13979 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL582835 13979 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983688 85488 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229923 85488 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
45481598 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197481 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573640 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
16126557 85428 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229764 85428 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983568 137556 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376581 137556 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
145965592 163864 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163864 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164177 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164177 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL437430 211970 0 None 3 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL452403 212229 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
145973990 164133 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372901 208561 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162666856 181892 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4786585 181892 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
10340786 70972 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL195746 70972 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
46897993 14274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1173172 14274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1200261 14274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
44409548 76976 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL208362 76976 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL573837 76976 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
46897999 14239 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1171808 14239 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200120 14239 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
15983558 141501 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL387661 141501 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
24953412 13970 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197628 13970 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL578853 13970 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
49799329 14273 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173171 14273 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200260 14273 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL412753 211276 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163134 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953058 13960 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197539 13960 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL575819 13960 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
15983684 85487 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229922 85487 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
24952349 13942 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197478 13942 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573570 13942 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
24952351 13952 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197508 13952 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574730 13952 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
15983695 144084 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL390792 144084 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983824 141504 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL387694 141504 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983566 85240 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228526 85240 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL501794 212374 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1165764 206787 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
145967082 163549 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL3104471 209317 5 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607809 214055 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
162666100 181687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783820 181687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163438 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983816 85417 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229709 85417 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164133 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164133 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44400855 134762 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL372689 134762 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
45482441 13943 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197479 13943 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573574 13943 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
24952709 13953 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197509 13953 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574731 13953 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953413 13964 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197568 13964 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL576922 13964 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
162658232 180406 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4758767 180406 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
45481583 13936 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197444 13936 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572467 13936 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
145967082 163549 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163549 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799366 14259 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172763 14259 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200218 14259 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
46897994 14284 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1173492 14284 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200286 14284 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
145978068 163184 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163184 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163438 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL508811 213366 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
49799023 14267 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173081 14267 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200246 14267 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
24952706 13941 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197477 13941 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573569 13941 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
162660720 180604 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 180604 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24955189 13935 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197443 13935 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL572454 13935 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL608097 214058 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
24952353 13937 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197454 13937 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572882 13937 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 163834 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163834 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11663047 1617 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
3501 1617 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
CHEMBL204989 1617 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
162656670 180336 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180336 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593612 214035 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
24952708 13931 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197439 13931 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572392 13931 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953057 13959 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197534 13959 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575630 13959 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
24955187 76365 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL206552 76365 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574304 76365 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
15983441 85218 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228411 85218 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145977587 163134 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163134 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL509604 213800 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162668785 182116 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789420 182116 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209317 5 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162662050 181265 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4778562 181265 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
49798989 14256 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172605 14256 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200194 14256 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799137 14293 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173725 14293 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200304 14293 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
25126427 2110 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2110 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2110 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
45487747 195209 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195209 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23728637 151190 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151190 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747296 170798 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 170798 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804161 91317 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91317 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10119117 87906 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 87906 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
23627613 195262 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 195262 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596967 195094 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195094 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 195449 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195449 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 195632 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195632 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747294 170500 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 170500 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
155543279 172724 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 172724 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747247 173482 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 173482 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45486911 195505 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 195505 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486917 195758 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 195758 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71717140 87900 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 87900 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
142747243 174163 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174163 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747265 175040 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175040 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
44596867 195295 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 195295 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486909 195469 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 195469 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71580034 87907 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 87907 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127070 196883 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196883 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24803165 88366 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236396 88366 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
142747268 171036 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171036 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
25127070 196883 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196883 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
155552384 173571 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 173571 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
142747256 175103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627556 196800 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 196800 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596965 195163 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195163 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25124736 196884 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196884 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71579840 87894 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 87894 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 87890 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 87890 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44597068 195095 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195095 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44206680 195326 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 195326 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
21023902 3479 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3479 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3479 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
44597069 195808 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195808 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25126424 195347 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195347 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71716535 87901 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 87901 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579748 87891 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 87891 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747285 173575 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 173575 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627554 195229 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 195229 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627555 196080 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 196080 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 195276 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195276 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
16656749 195446 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195446 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195488 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195488 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25128051 196015 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 196015 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 196884 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196884 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747253 170537 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 170537 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
10173280 2946 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2946 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2946 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
2164 3470 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3470 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3470 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
45486918 195572 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568388 195572 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627492 195182 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 195182 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
71717139 87897 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 87897 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24803990 91363 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL241128 91363 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627612 196135 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196135 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71719581 87895 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87895 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127071 196882 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196882 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
44596965 195163 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195163 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627305 195757 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 195757 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627251 197241 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 197241 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579743 87886 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87886 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720175 87904 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 87904 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24804323 90389 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90389 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597068 195095 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195095 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195488 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195488 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45487731 196886 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196886 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747289 170024 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170024 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 170820 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 170820 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627722 195528 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195528 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24803168 89462 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237877 89462 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627249 195558 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195558 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804816 145860 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 145860 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747251 171924 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 171924 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 172878 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 172878 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597398 195123 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195123 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
155512483 169098 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169098 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
23627722 195528 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195528 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125422 195611 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195611 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
16656749 195446 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195446 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486908 195217 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 195217 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71718372 87899 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 87899 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
142747255 170875 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 170875 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
10173280 2946 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2946 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2946 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
44597071 196885 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196885 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
142747273 171511 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 171511 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804324 89464 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89464 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
21023902 3479 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3479 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3479 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
25128051 196015 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 196015 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
71580134 87911 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 87911 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44596967 195094 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195094 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747298 172684 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 172684 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597070 195098 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195098 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
10173280 2946 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
3516 2946 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
CHEMBL567303 2946 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
71719581 87895 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87895 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24893978 995 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 995 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 995 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
25127072 196061 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196061 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
45487748 196073 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196073 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596964 195276 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195276 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 195263 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195263 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
24804326 144817 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 144817 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597070 195098 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195098 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
11272107 87885 37 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 87885 37 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24803167 89463 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237878 89463 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
23627430 195218 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566145 195218 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 195449 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195449 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747254 169938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 169938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579743 87886 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87886 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747238 174961 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 174961 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45487747 195209 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195209 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 195263 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195263 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
25127071 196882 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196882 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25067560 187388 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187388 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
45487731 196886 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196886 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25127072 196061 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196061 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24804325 144821 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 144821 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90453 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90453 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
25125422 195611 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195611 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
71718978 87903 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 87903 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
71580033 87908 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348525 87908 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25125764 195515 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195515 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 195515 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195515 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44597071 196885 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196885 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
71579743 87886 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87886 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24804491 89524 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89524 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
71719582 87905 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 87905 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579843 87896 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 87896 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
45487748 196073 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196073 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
10120078 67300 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67300 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448692 94457 3 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94457 3 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
71719581 87895 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87895 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486916 195567 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568358 195567 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597398 195123 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195123 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25126424 195347 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195347 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125075 196060 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 196060 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747291 169333 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169333 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747279 173936 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 173936 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627557 195269 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 195269 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24802993 88820 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236800 88820 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71579744 87887 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 87887 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486910 195700 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 195700 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 195632 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195632 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579935 87898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 87898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
25126427 2110 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2110 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2110 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
21023902 3479 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3479 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3479 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
142747275 169079 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169079 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747242 169967 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 169967 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174393 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174393 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
23627249 195558 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195558 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597069 195808 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195808 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23627612 196135 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196135 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125075 196060 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 196060 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
148470142 169110 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169110 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747258 173242 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173242 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747281 175378 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175378 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44435003 145832 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392142 145832 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71720174 87902 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 87902 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
25067045 154970 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154970 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL387916 210666 0 None - 0 Rat 8.0 pKd = 8 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
25067560 187388 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187388 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580475 192617 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192617 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 187435 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187435 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580519 187301 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187301 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 187754 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187754 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL389653 210684 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 207701 10 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL389654 210685 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL218698 207653 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist potency against human urotensin-2-induced contraction of rat aortic ringAntagonist potency against human urotensin-2-induced contraction of rat aortic ring
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
2164 3470 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3470 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3470 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
44206682 10378 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL1165145 10378 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195326 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195326 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195326 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195326 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
46907359 10364 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10364 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
11663047 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
11663047 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
3501 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
3501 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
CHEMBL204989 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
CHEMBL204989 1617 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
9441 3893 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27791374
9436 103 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12943190
2163 3396 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
9803617 3396 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
CHEMBL93758 3396 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
10173280 2946 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
3516 2946 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
CHEMBL567303 2946 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
10886 3606 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720777 3606 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720778 3606 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
11438 1458 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
46862051 1458 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
11995575 3898 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
2156 3898 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
CHEMBL437110 3898 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283


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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
CHEMBL3315148 209626 0 None - 1 Rat 10.9 pEC50 = 10.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315144 209622 0 None - 1 Rat 10.7 pEC50 = 10.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315139 209617 9 None - 1 Rat 9.4 pEC50 = 9.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 209630 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 209618 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315146 209624 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 211970 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL437430 211970 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3315150 209628 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137628790 160449 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160449 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160449 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177635 120694 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120694 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 120694 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120694 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051713 140497 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 140497 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 207658 0 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630764 160557 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 160557 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 160557 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 160585 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 160585 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 160585 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177633 120692 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120692 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629788 160633 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 160633 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 160633 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177633 120692 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120692 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 160619 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 160645 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629789 160634 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 160634 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 160634 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 160619 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
44409478 75584 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205157 75584 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
155519842 169807 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 169807 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
15983315 76992 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL208436 76992 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11640431 140827 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383698 140827 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629655 160619 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 120684 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120684 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631060 160608 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 160608 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 160608 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 120684 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120684 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120686 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120686 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120686 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120686 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
2151 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
9797568 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
CHEMBL192359 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
11626617 77007 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL208536 77007 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
15983313 97808 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL274508 97808 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983200 77005 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL208512 77005 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL3104463 209313 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11684574 165483 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL425592 165483 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104463 209313 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 160655 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 160619 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629651 160614 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 160614 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 160614 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177624 120683 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120683 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 120683 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120683 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315149 209627 0 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
15983196 193923 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL555609 193923 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631008 160595 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 160595 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 160595 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
127050201 140408 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140408 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155544020 172743 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172743 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629875 160644 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 160644 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 160644 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
11325792 139637 8 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
CHEMBL380346 139637 8 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
11559579 74416 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL203106 74416 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
11631605 74705 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL203531 74705 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11546868 75607 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205254 75607 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983325 138177 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377946 138177 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
137631155 160655 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11552098 74659 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203337 74659 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11625650 76411 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206811 76411 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
44409467 74406 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203080 74406 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL572699 74406 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629875 160644 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 160644 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 160644 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127049894 140430 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140430 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137628890 160427 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160427 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160427 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
44409534 75206 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204516 75206 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
11546571 75629 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL205430 75629 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL3104461 209311 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 160655 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 160585 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 160585 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 160585 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104461 209311 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11674961 139818 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL380745 139818 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11508921 76821 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207882 76821 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11569119 75927 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205859 75927 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11566781 76274 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206371 76274 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631154 160654 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11510666 140186 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL381756 140186 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL3315143 209621 0 None - 1 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
121335724 158398 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158398 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
155560750 174509 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174509 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104460 209310 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11591072 138184 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377973 138184 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983317 75123 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL204227 75123 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
122177634 120693 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120693 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629651 160614 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 160614 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 160614 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137641820 160679 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 160679 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 160679 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11531958 140767 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383326 140767 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11524599 76374 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206596 76374 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983311 138361 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL378235 138361 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 160645 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155532198 171174 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171174 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2151 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11532525 75700 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL205735 75700 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11573773 140533 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382477 140533 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
127052350 140467 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140467 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177625 120684 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120684 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315147 209625 0 None - 1 Rat 8.6 pEC50 = 8.6 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
155537097 171690 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171690 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104471 209317 5 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177625 120684 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120684 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104465 209315 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11697064 76384 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206661 76384 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104465 209315 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177629 120688 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120688 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177629 120688 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120688 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104464 209314 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11559558 75674 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205628 75674 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
11495815 76375 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206597 76375 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11595438 77308 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL208886 77308 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
137631155 160655 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104464 209314 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155532198 171174 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171174 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137631154 160654 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11681737 75625 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205390 75625 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983323 76394 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206719 76394 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
122177624 120683 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120683 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 120683 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120683 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537097 171690 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171690 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
121335724 158398 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158398 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL3104462 209312 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11526048 74351 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203051 74351 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104462 209312 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
2151 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
15983321 75182 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204368 75182 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104467 209316 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11627432 74703 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203528 74703 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11501947 75678 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205681 75678 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983198 140756 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL383258 140756 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11648503 76364 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206551 76364 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11609885 140504 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL382401 140504 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL593662 214036 9 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL593662 214036 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630539 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL593662 214036 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137629890 160465 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 160465 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 160465 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631008 160595 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 160595 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 160595 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 160645 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631154 160654 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
135747623 174493 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174493 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137641820 160679 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 160679 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 160679 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 120693 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120693 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630539 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 160528 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140417 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140417 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 207658 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
135747623 174493 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174493 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630689 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177631 120690 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120690 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 120690 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120690 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628790 160449 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160449 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160449 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631060 160608 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 160608 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 160608 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 160474 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 160474 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 160474 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630764 160557 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 160557 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 160557 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127051713 140497 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 140497 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3315141 209619 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
137630124 160501 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 160501 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 160501 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 160645 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 160522 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 160522 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 160522 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
2151 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11696838 76803 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207823 76803 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL573857 76803 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3315145 209623 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
11537255 74092 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL202725 74092 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11582902 75597 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL205201 75597 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 160645 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104460 209310 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11604535 75645 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205488 75645 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
122177629 120688 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120688 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628942 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630802 160564 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 160564 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 160564 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
137631155 160655 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 160609 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177630 120689 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120689 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177630 120689 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120689 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 160619 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155567837 175463 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 175463 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629789 160634 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 160634 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 160634 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 120693 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120693 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120693 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120691 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120691 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120691 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120691 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155524087 170326 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170326 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
122177629 120688 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120688 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628889 160426 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160426 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160426 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140417 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140417 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177631 120690 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120690 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 120690 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120690 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155536007 171560 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 171560 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628942 160437 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160437 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160437 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177636 120695 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120695 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104644 209323 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104644 209323 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
44409477 76794 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207783 76794 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11496131 139809 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL380704 139809 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
15983319 76419 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL206832 76419 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
122177636 120695 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120695 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315142 209620 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
137629655 160619 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160619 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160619 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 160474 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 160474 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 160474 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630124 160501 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 160501 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 160501 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629788 160633 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 160633 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 160633 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629877 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127051389 140462 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140462 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155529504 170866 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170866 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155524087 170326 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170326 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218994 207658 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629877 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 160646 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177628 120687 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120687 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 120687 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120687 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 171780 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171780 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177632 120691 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120691 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120691 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120691 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 171780 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171780 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628889 160426 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160426 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160426 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
44409548 76976 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL208362 76976 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL573837 76976 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 209320 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11525327 140566 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382688 140566 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11653844 75044 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203937 75044 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11524788 76161 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205991 76161 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104637 209318 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155560750 174509 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174509 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104637 209318 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137628890 160427 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160427 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160427 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 160645 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160645 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160645 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 160522 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 160522 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 160522 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631154 160654 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177627 120686 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120686 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120686 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120686 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630802 160564 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 160564 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 160564 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177626 120685 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120685 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 120685 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120685 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
11496252 138175 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL377938 138175 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11567714 74801 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203626 74801 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104471 209317 5 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631154 160654 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL3104471 209317 5 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629890 160465 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 160465 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 160465 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177628 120687 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120687 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 120687 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120687 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051389 140462 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140462 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
11663047 1617 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
3501 1617 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
CHEMBL204989 1617 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
11589093 75563 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204988 75563 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
122177630 120689 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120689 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104471 209317 5 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177630 120689 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120689 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 120695 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120695 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 120695 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120695 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631154 160654 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160654 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160654 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630689 160552 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 160552 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 160552 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177635 120694 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120694 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 120692 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120692 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 120694 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120694 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 120692 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120692 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104638 209319 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155544020 172743 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172743 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104467 209316 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 209319 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
24955187 76365 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL206552 76365 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL574304 76365 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 209320 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
127052350 140467 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140467 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137631155 160655 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160655 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160655 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177626 120685 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120685 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 120685 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120685 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155529504 170866 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170866 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
127049894 140430 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140430 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
127050201 140408 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140408 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155520913 169968 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 169968 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44189349 181213 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181213 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104464 209314 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134134886 143937 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3906682 143937 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
134155324 150403 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3957806 150403 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
156012877 176867 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638745 176867 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162657061 180318 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180318 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209317 5 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156017817 177255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4643905 177255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104471 209317 5 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155552384 173571 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 173571 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
134156076 150764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3960613 150764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
71579840 87894 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 87894 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86291695 115758 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358677 115758 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
71579744 87887 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 87887 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL437430 211970 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86292101 115766 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358687 115766 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL437430 211970 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134152840 152978 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
CHEMBL3979822 152978 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
10119117 87906 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 87906 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
156016806 177150 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642313 177150 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71579748 87891 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 87891 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747255 170875 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 170875 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
123185525 142908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3898238 142908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134133034 144006 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3907266 144006 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
86291907 115762 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
CHEMBL3358683 115762 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
142747275 169079 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169079 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747296 170798 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 170798 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747256 175103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747281 175378 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175378 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
156013999 176622 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635150 176622 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162648628 179275 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179275 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
2164 3470 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3470 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3470 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL3104637 209318 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580034 87907 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 87907 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86305736 115749 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358667 115749 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
162671682 182307 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182307 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104637 209318 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747285 173575 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 173575 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747265 175040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
71719582 87905 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 87905 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
134156326 153750 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3986509 153750 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104640 209321 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104640 209321 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104471 209317 5 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
86291908 115763 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
CHEMBL3358684 115763 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
162646037 178934 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 178934 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
156014461 176616 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635039 176616 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
142747247 173482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 173482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291906 115761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
CHEMBL3358682 115761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
86291904 115764 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358685 115764 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104465 209315 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104465 209315 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580135 87912 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348529 87912 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723010 115752 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358670 115752 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
71719581 87895 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87895 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723009 115751 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358669 115751 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
11272107 87885 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 87885 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 87890 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 87890 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747254 169938 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 169938 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 172878 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 172878 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579745 87888 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348504 87888 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134151496 152691 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3977330 152691 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
142747291 169333 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169333 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291696 115759 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358679 115759 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
145966260 163834 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163834 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
142747243 174163 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174163 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174393 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174393 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL3104463 209313 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71720175 87904 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 87904 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL3104643 209322 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104643 209322 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 209312 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104463 209313 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 209312 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156016802 177146 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642307 177146 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
10173280 2946 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2946 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2946 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
145978068 163184 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163184 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 180711 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 180711 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162660720 180604 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 180604 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579839 87893 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348509 87893 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747279 173936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 173936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134148271 149408 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3949719 149408 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
86291694 115757 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358676 115757 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
142747238 174961 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 174961 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747253 170537 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 170537 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
71579743 87886 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87886 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134153111 152029 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
CHEMBL3971737 152029 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
71579843 87896 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 87896 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
86292104 115754 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358672 115754 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
156010342 176499 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4633010 176499 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104459 209309 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104459 209309 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747273 171511 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 171511 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 170820 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 170820 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291905 115765 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358686 115765 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
155512483 169098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169098 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
162656670 180336 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180336 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579746 87889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348505 87889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720174 87902 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 87902 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
118723011 115753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358671 115753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104638 209319 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 209319 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
148470142 169110 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169110 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747289 170024 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170024 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
162670598 182340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182340 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162677235 182913 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 182913 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
123794584 151760 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3969435 151760 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134152171 152680 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977271 152680 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3104471 209317 5 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
145977223 163438 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163438 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164177 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164177 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
134133573 142717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3896625 142717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
71579935 87898 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 87898 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
71718978 87903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 87903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
134141359 146263 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3924660 146263 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
134142270 145092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3915656 145092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104639 209320 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104639 209320 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747294 170500 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 170500 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
21023902 3479 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3479 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3479 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
142747268 171036 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171036 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104461 209311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86291697 115760 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358680 115760 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3104461 209311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162651887 179691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 179691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
86305831 115750 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
CHEMBL3358668 115750 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
142747251 171924 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 171924 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134140417 145746 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3920751 145746 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
71716535 87901 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 87901 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580035 87909 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348526 87909 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134141963 146464 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3926450 146464 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
142747298 172684 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 172684 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579838 87892 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348508 87892 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
10303115 10327 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
CHEMBL1163360 10327 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
142747258 173242 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173242 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71717140 87900 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 87900 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
156012366 176833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638346 176833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71718372 87899 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 87899 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
134151328 151700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3968841 151700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
123922871 152752 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977836 152752 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
134146007 148437 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
CHEMBL3942137 148437 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
86294592 115756 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
CHEMBL3358674 115756 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
162668637 182065 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182065 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104644 209323 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
123264706 142829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3897677 142829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
71580134 87911 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 87911 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL3104460 209310 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104460 209310 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71717139 87897 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 87897 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580133 87910 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348527 87910 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134142581 145096 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3915670 145096 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
134156353 153828 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3987058 153828 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104467 209316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104467 209316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162644923 178849 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 178849 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
155543279 172724 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 172724 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104644 209323 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134151441 152855 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3978782 152855 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
142747242 169967 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 169967 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
118723012 115755 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358673 115755 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
134138102 147324 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL3933152 147324 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL1165797 206792 0 None - 1 Rat 10.7 pKi = 10.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL577772 214000 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 214000 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1163463 206777 6 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 210690 1 None - 1 Human 9.7 pKi = 9.7 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL390094 210690 1 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL390094 210690 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL390094 210690 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315139 209617 9 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL426020 211595 0 None - 1 Human 9.6 pKi = 9.6 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL426020 211595 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL426020 211595 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL426020 211595 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL218994 207658 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL504097 212403 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44561239 173134 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453587 173134 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL3315142 209620 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44449106 94670 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255509 94670 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
44449079 95019 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
CHEMBL257171 95019 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
44449053 94972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256989 94972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL3315141 209619 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315148 209626 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 211970 0 None - 1 Human 9.1 pKi = 9.1 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL437430 211970 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL437430 211970 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL437430 211970 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509604 213800 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL593662 214036 9 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL510618 213809 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2371933 208410 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44449004 95074 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL257415 95074 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL3315147 209625 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL385281 210599 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44448876 94660 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255462 94660 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL218994 207658 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315146 209624 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370836 208187 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2370836 208187 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm0309912
CHEMBL224616 207704 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL388060 210667 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL374468 210454 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CN[C@@H](CC(=O)O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0602110
CHEMBL448403 212206 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155536007 171560 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 171560 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
135747623 174493 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174493 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3315144 209622 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 209630 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315150 209628 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 209618 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
44580517 187436 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497562 187436 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580475 192617 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192617 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
25067045 154970 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154970 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL412179 211227 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL389654 210685 0 None 5 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44568398 182952 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479994 182952 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448290 94927 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256773 94927 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
44580679 187418 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497368 187418 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580518 187473 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL497765 187473 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44399254 67294 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190501 67294 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580519 187301 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187301 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 187754 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187754 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44448714 95064 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257365 95064 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44568339 183267 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480776 183267 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44534500 193336 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
CHEMBL548340 193336 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
25127071 196882 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196882 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 196884 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196884 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL509042 213488 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
10120078 67300 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL190533 67300 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL1163479 206783 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46907359 10364 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10364 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
10190075 188172 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL505360 188172 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL3315151 209629 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370837 208188 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2372643 208533 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm0309912
44580564 187220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495907 187220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580476 187227 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187227 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
12704866 187754 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187754 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL387916 210666 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL3315145 209623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
44597398 195123 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195123 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44568429 190171 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL518312 190171 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
10278166 3472 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
3531 3472 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
CHEMBL1164033 3472 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
10120078 67300 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67300 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399063 68287 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191793 68287 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580475 192617 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192617 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448653 171167 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
CHEMBL446717 171167 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
44561196 172941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453074 172941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44593421 186120 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488470 186120 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
23627666 195449 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195449 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL508811 213366 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44449136 154721 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402813 154721 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44596966 195632 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195632 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL415851 211457 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0602110
24804491 89524 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89524 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10210584 183476 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482302 183476 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
45486917 195758 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 195758 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561123 192891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL527199 192891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1165794 206790 1 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44597071 196885 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196885 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568399 191985 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521418 191985 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448469 94752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL255927 94752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
25067046 154633 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154633 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL389653 210684 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL500949 212358 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44596869 195263 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195263 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
44534506 183471 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482258 183471 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155540766 171941 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4483461 171941 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL425467 211588 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10230399 122836 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL361664 122836 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448314 168190 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
CHEMBL437216 168190 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
44580476 187227 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187227 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448691 94456 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254153 94456 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448337 94802 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256159 94802 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580436 171862 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL447747 171862 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448775 94493 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254356 94493 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561197 172942 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453075 172942 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44448775 94493 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL254356 94493 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44597068 195095 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195095 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL3315153 209631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
24804325 144821 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 144821 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627554 195229 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 195229 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627556 196800 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 196800 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44448691 94456 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254153 94456 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1163471 206779 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
25126424 195347 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195347 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 195515 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195515 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568526 189955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL517991 189955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL376223 210496 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501579 212369 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44580563 192535 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522895 192535 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
12052419 67688 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191401 67688 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580473 187355 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187355 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448474 94797 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256140 94797 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448317 94875 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
CHEMBL256516 94875 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
44448514 154904 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403833 154904 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399475 67248 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL190137 67248 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399166 170445 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL445655 170445 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448549 95217 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL258017 95217 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL375241 210468 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44449228 95156 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL257767 95156 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44449107 154666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL402520 154666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
155544020 172743 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172743 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218825 207656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)C(C)(C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315149 209627 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL265166 208894 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c([N+](=O)[O-])c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL524855 213846 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL216712 207595 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
155567837 175463 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 175463 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL266651 208945 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44561157 186138 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488642 186138 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
155537736 171780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171780 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2164 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL1163475 206781 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
23627305 195757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 195757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
2164 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3470 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
155550733 173712 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4549818 173712 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
155524911 170351 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4455086 170351 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL505288 212420 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155537097 171690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155560750 174509 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174509 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL219356 207667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627555 196080 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 196080 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534510 182950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479993 182950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155519842 169807 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 169807 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
45487731 196886 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196886 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44448510 95060 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257337 95060 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580519 187301 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187301 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
44580437 188490 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL509831 188490 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44561156 186136 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488635 186136 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
2164 3470 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3470 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3470 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399168 134663 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372019 134663 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448431 95104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257563 95104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399476 67165 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL189482 67165 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
44399169 135059 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL372911 135059 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399083 159501 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL410825 159501 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399234 161311 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL414847 161311 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580515 187435 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187435 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44448394 154668 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402543 154668 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580477 188189 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505617 188189 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505358 212421 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
11995575 3898 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
2156 3898 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
CHEMBL437110 3898 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
24804324 89464 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89464 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44596867 195295 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 195295 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486910 195700 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 195700 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561240 172046 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL449192 172046 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
44561238 172938 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453067 172938 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44449052 94971 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256988 94971 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
10121972 182472 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL479413 182472 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
2164 3470 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3470 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3470 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
155524087 170326 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170326 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155529504 170866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL507406 212539 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
25067045 154970 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154970 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067560 187388 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187388 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580472 187389 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187389 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
24804323 90389 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90389 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90453 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90453 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44448513 94702 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255665 94702 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448471 94796 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256138 94796 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448338 94803 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256160 94803 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580683 187448 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497580 187448 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
23627492 195182 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 195182 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
23627613 195262 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 195262 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627557 195269 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 195269 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96327 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL264726 96327 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580634 187224 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495920 187224 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3470 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3470 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3470 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399453 67484 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190975 67484 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448361 160907 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL412746 160907 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
44448734 168437 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
CHEMBL439244 168437 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
44596965 195163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96327 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL264726 96327 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
23627251 197241 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 197241 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 195276 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195276 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568226 183019 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL480170 183019 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
44568368 183470 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482257 183470 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44568426 191069 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
CHEMBL519629 191069 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
44568484 183425 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481964 183425 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44399062 69048 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193133 69048 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399093 126879 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365966 126879 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399084 133092 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL371361 133092 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580472 187389 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187389 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448736 94410 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253749 94410 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448692 94457 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94457 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL439551 212099 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44448732 94381 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253540 94381 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580632 187223 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
CHEMBL495919 187223 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
24863522 188320 9 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL507691 188320 9 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
10173280 2946 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2946 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2946 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
25126427 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
25125422 195611 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195611 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
24893978 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL1165796 206791 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL218994 207658 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448913 155009 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL404289 155009 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
11691 1948 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
3082718 1948 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL38576 1948 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL218698 207653 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10173280 2946 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2946 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2946 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
10119115 190165 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518301 190165 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
44568428 183018 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480165 183018 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
24804816 145860 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 145860 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
45486909 195469 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 195469 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127072 196061 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196061 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568370 189246 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL516606 189246 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
16656749 195446 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195446 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534490 193303 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
CHEMBL546011 193303 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
155520913 169968 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 169968 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44597070 195098 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195098 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
23627722 195528 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195528 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10173280 2946 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2946 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2946 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
44561276 173021 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453329 173021 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448976 94915 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL256721 94915 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
44448947 95015 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL257150 95015 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL223905 207701 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 207701 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL223905 207701 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
21023902 3479 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
2165 3479 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
CHEMBL522770 3479 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
44568369 183472 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482259 183472 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448339 94840 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256365 94840 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580631 187222 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187222 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
44580682 187446 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497579 187446 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
18613636 183311 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL481129 183311 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
12052410 67608 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191110 67608 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052411 68834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL192552 68834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052408 125860 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365053 125860 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448656 94586 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254994 94586 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448293 94928 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
CHEMBL256774 94928 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
155560178 174359 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4565187 174359 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
24804326 144817 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 144817 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
45486911 195505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 195505 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627612 196135 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196135 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195488 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195488 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127070 196883 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196883 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
25067046 154633 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL402303 154633 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561237 187662 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL499582 187662 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448874 94659 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255460 94659 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
44449202 95264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL258251 95264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL3104471 209317 5 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
25067046 154633 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154633 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580473 187355 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187355 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 187435 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187435 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
25067046 154633 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154633 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL452403 212229 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315143 209621 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44534504 183266 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL480775 183266 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL1163477 206782 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
45487747 195209 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195209 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568400 183421 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481946 183421 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448359 95061 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257349 95061 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580681 187445 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497578 187445 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
25211348 188171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
CHEMBL505353 188171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
44561195 172645 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL452298 172645 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561236 172821 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL452808 172821 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
12052412 69038 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193033 69038 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399398 69057 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
CHEMBL193266 69057 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
44399094 121841 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
CHEMBL359993 121841 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
12052415 134758 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372658 134758 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580631 187222 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187222 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
25067560 187388 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187388 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448428 94701 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255664 94701 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44206680 195326 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195326 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195326 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 195326 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
23728637 151190 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151190 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44568427 183443 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482114 183443 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL593662 214036 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448472 154931 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403947 154931 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067045 154970 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154970 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
45486908 195217 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 195217 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10232516 191949 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521117 191949 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL428990 211741 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(=O)O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627249 195558 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195558 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804161 91317 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91317 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44448772 154718 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402805 154718 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44448315 94828 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256299 94828 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
44448316 94829 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256300 94829 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448429 154634 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402304 154634 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580633 187047 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL494934 187047 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580565 192800 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL525759 192800 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
12052413 67173 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL189525 67173 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448733 94409 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253747 94409 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448586 95100 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257552 95100 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448289 154991 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
CHEMBL404244 154991 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
44580680 187419 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497369 187419 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580630 192143 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522074 192143 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580474 192458 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522381 192458 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448657 94587 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254995 94587 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
44448396 95025 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257187 95025 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44449171 94963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL256937 94963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
21023902 3479 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3479 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3479 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
45487748 196073 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196073 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
155532198 171174 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171174 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44596967 195094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL383996 210568 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501794 212374 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509009 213468 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL504723 212411 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44597069 195808 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195808 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568309 190612 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518949 190612 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
11439 3243 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
155817517 3243 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
2161 115 0 None - 1 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
11995575 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
11995575 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2156 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
2156 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
CHEMBL437110 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
CHEMBL437110 3898 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2162 642 0 None - 1 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12770925
2166 3783 0 None - 1 Human 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
24893978 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
8872 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
CHEMBL495075 995 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
9439 894 0 None - 1 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17125276
2151 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
2151 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
9797568 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
9797568 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
CHEMBL192359 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
CHEMBL192359 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
10278166 3472 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
3531 3472 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
CHEMBL1164033 3472 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
2164 3470 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
9846574 3470 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
CHEMBL366221 3470 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
134813899 2920 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
9438 2920 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
21023902 3479 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3479 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3479 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2167 3885 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14645137
25126427 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
9437 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
CHEMBL567713 2110 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
2153 3896 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10499587
2153 3896 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10548501
2153 3896 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10559967
2153 3896 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10581185
10213684 3872 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2152 3872 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
CHEMBL414256 3872 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2160 2993 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
21023902 3479 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
21023902 3479 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3479 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3479 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3479 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3479 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2154 3895 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2154 3895 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3895 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3897 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3896 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2153 3896 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3897 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2155 3897 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3896 0 None 1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3895 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3897 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2159 750 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12495432