Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL218994 211862 None 0 Rat Functional pEC50 = 10 10.0 1 2
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 210986 None 0 Rat Functional pEC50 = 10.0 10.0 - 1
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 210977 None 0 Rat Functional pEC50 = 9.8 9.8 - 1
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 210978 None 6 Rat Functional pEC50 = 9.8 9.8 - 1
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 214897 None 0 Rat Functional pEC50 = 9.6 9.6 - 1
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 210979 None 0 Rat Functional pEC50 = 9.5 9.5 - 1
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 210993 None 0 Rat Functional pEC50 = 9.5 9.5 - 1
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 210989 None 0 Rat Functional pEC50 = 9.4 9.4 - 1
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 181901 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 181901 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 218267 None 0 Rat Functional pEC50 = 9.3 9.3 - 1
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 218267 None 0 Rat Functional pEC50 = 9.3 9.3 - 1
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 210987 None 0 Rat Functional pEC50 = 9.2 9.2 - 1
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 216662 None 0 Rat Functional pEC50 = 9.2 9.2 - 1
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 210981 None 0 Rat Functional pEC50 = 9.1 9.1 - 1
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 180196 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 180196 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 216179 None 0 Human Functional pEC50 = 9.0 9.0 -3 2
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 164511 None 0 Rat Functional pEC50 = 9.0 9.0 33 2
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 164511 None 0 Rat Functional pEC50 = 9.0 9.0 33 2
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 164780 None 0 Rat Functional pEC50 = 8.9 8.9 181 2
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 164780 None 0 Rat Functional pEC50 = 8.9 8.9 181 2
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 218112 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 218075 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 179620 None 0 Human Functional pEC50 = 8.8 8.8 1737 6
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 179620 None 0 Human Functional pEC50 = 8.8 8.8 1737 6
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 210992 None 0 Rat Functional pEC50 = 8.8 8.8 - 1
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 210990 None 0 Rat Functional pEC50 = 8.8 8.8 - 1
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 210991 None 0 Rat Functional pEC50 = 8.8 8.8 - 1
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 212763 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 214818 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 218198 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 212762 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 164196 None 0 Rat Functional pEC50 = 8.7 8.7 416 2
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 164196 None 0 Rat Functional pEC50 = 8.7 8.7 416 2
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 182123 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 182123 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 179961 None 0 Human Functional pEC50 = 8 8.0 - 1
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 179961 None 0 Human Functional pEC50 = 8 8.0 - 1
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 218304 None 0 Human Functional pEC50 = 8 8.0 - 1
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 179535 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 179535 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 163831 None 0 Rat Functional pEC50 = 8.0 8.0 1 2
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 163831 None 0 Rat Functional pEC50 = 8.0 8.0 1 2
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 164824 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 164824 None 0 Human Functional pEC50 = 8.0 8.0 1 2
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 215075 None 0 Human Functional pEC50 = 6 6.0 - 1
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 216680 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
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 180803 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 180803 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14088 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14088 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14088 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 182753 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 182753 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14073 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14073 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14073 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14070 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14070 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14070 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 181404 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 181404 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 164085 None 0 Rat Functional pEC50 = 7.0 7.0 1 2
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 164085 None 0 Rat Functional pEC50 = 7.0 7.0 1 2
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 244 None 10 Human Functional pEC50 = 6.0 6.0 -2 2
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 244 None 10 Human Functional pEC50 = 6.0 6.0 -2 2
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 244 None 10 Human Functional pEC50 = 6.0 6.0 -2 2
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 85681 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 85681 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 85700 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 85700 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 10848 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 10848 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14388 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14388 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14388 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164196 None 0 Human Functional pEC50 = 5.9 5.9 -416 2
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 164196 None 0 Human Functional pEC50 = 5.9 5.9 -416 2
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 164085 None 0 Rat Functional pEC50 = 6.9 6.9 1 2
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 164085 None 0 Rat Functional pEC50 = 6.9 6.9 1 2
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 14371 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14371 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14371 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 164511 None 0 Rat Functional pEC50 = 7.9 7.9 33 2
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 164511 None 0 Rat Functional pEC50 = 7.9 7.9 33 2
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 218323 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 163781 None 0 Rat Functional pEC50 = 7.9 7.9 14 2
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 163781 None 0 Rat Functional pEC50 = 7.9 7.9 14 2
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 14068 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 14068 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 14068 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 164085 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 164085 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 164085 None 0 Rat Functional pEC50 = 6.9 6.9 1 2
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 164085 None 0 Rat Functional pEC50 = 6.9 6.9 1 2
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 164511 None 0 Human Functional pEC50 = 6.9 6.9 -33 2
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 164511 None 0 Human Functional pEC50 = 6.9 6.9 -33 2
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 14057 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 14057 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 14057 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 85689 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 85689 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 218324 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 163781 None 0 Rat Functional pEC50 = 7.9 7.9 14 2
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 163781 None 0 Rat Functional pEC50 = 7.9 7.9 14 2
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 212769 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 140254 None 7 Human Functional pEC50 = 6.9 6.9 - 1
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 140254 None 7 Human Functional pEC50 = 6.9 6.9 - 1
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 85880 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 85880 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182378 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182378 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 14391 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14391 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 14391 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 161841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 182320 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 182320 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 213522 None 7 Human Functional pEC50 = 6.8 6.8 -1 2
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 74781 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 74781 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 74781 None 1 Human Functional pEC50 = 5.8 5.8 - 1
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 14401 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 14401 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 14401 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164481 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 164481 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
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 212768 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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 164085 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 164085 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
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 182995 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 182995 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 137421 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 137421 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 138173 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 138173 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 180173 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 180173 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164085 None 0 Rat Functional pEC50 = 7.8 7.8 1 2
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 164085 None 0 Rat Functional pEC50 = 7.8 7.8 1 2
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 218327 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 85680 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 85680 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 164780 None 0 Rat Functional pEC50 = 7.8 7.8 181 2
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 164780 None 0 Rat Functional pEC50 = 7.8 7.8 181 2
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 14375 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 14375 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 14375 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 169496 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 169496 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 182835 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 182835 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 164824 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 164824 None 0 Human Functional pEC50 = 6.7 6.7 1 2
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 76755 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 76755 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 163831 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 163831 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
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 212767 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 14395 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14395 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14395 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14051 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 14051 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 14051 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 85950 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 85950 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 210980 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 213363 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 215819 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 215161 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 215804 None 0 Rat Functional pEC50 = 8.6 8.6 - 1
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 212761 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 164196 None 0 Rat Functional pEC50 = 8.6 8.6 416 2
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 164196 None 0 Rat Functional pEC50 = 8.6 8.6 416 2
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 218326 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 182139 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 182139 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 14058 None 2 Human Functional pEC50 = 7.6 7.6 - 1
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 14058 None 2 Human Functional pEC50 = 7.6 7.6 - 1
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 14058 None 2 Human Functional pEC50 = 7.6 7.6 - 1
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 14360 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14360 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14360 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 14369 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14369 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14369 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 85906 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 85906 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 183028 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183028 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 212760 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14392 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14392 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14392 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 183601 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 183601 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 244 None 10 Human Functional pEC50 = 6.6 6.6 -2 2
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 244 None 10 Human Functional pEC50 = 6.6 6.6 -2 2
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 244 None 10 Human Functional pEC50 = 6.6 6.6 -2 2
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 210983 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 14368 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14368 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 14368 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 164481 None 0 Human Functional pEC50 = 7.6 7.6 -2 2
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 164481 None 0 Human Functional pEC50 = 7.6 7.6 -2 2
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 14067 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14067 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 14067 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 164085 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 164085 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 14402 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14402 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14402 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 180644 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 180644 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 14380 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14380 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14380 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 85688 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 85688 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 3935 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 3935 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 3935 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 212770 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 163781 None 0 Rat Functional pEC50 = 8.5 8.5 14 2
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 163781 None 0 Rat Functional pEC50 = 8.5 8.5 14 2
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 212766 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 211270 None 0 Human Functional pEC50 = 8.5 8.5 -102 8
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 181006 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 181006 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 211785 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 213522 None 7 Human Functional pEC50 = 8.4 8.4 -1 2
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 180018 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 180018 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 214830 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 179934 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 179934 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 244 None 10 Human Functional pEC50 = 6.5 6.5 -2 2
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 244 None 10 Human Functional pEC50 = 6.5 6.5 -2 2
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 244 None 10 Human Functional pEC50 = 6.5 6.5 -2 2
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 14049 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14049 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14049 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 85854 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 85854 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 210982 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
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 164824 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 164824 None 0 Rat Functional pEC50 = 7.5 7.5 -1 2
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 14082 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14082 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14082 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 77185 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 77185 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 77185 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 164481 None 0 Rat Functional pEC50 = 7.5 7.5 2 2
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 164481 None 0 Rat Functional pEC50 = 7.5 7.5 2 2
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 181399 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 181399 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 181897 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 181897 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164780 None 0 Human Functional pEC50 = 5.5 5.5 -181 2
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 164780 None 0 Human Functional pEC50 = 5.5 5.5 -181 2
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 14077 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14077 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 14077 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 164511 None 0 Human Functional pEC50 = 6.5 6.5 -33 2
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 164511 None 0 Human Functional pEC50 = 6.5 6.5 -33 2
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 14052 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14052 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 14052 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 164085 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 164085 None 0 Rat Functional pEC50 = 7.5 7.5 1 2
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 163781 None 0 Human Functional pEC50 = 6.5 6.5 -14 2
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 163781 None 0 Human Functional pEC50 = 6.5 6.5 -14 2
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 164196 None 0 Human Functional pEC50 = 5.5 5.5 -416 2
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 164196 None 0 Human Functional pEC50 = 5.5 5.5 -416 2
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 163831 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 163831 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
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 14063 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14063 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14063 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 210984 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 85879 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85879 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 164780 None 0 Human Functional pEC50 = 6.4 6.4 -181 2
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 164780 None 0 Human Functional pEC50 = 6.4 6.4 -181 2
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 85881 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85881 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14065 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14065 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14065 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14408 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14408 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14408 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 85690 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85690 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 218303 None 7 Human Functional pEC50 = 8.4 8.4 -1 2
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 180377 None 0 Human Functional pEC50 = 8.3 8.3 112 5
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 180377 None 0 Human Functional pEC50 = 8.3 8.3 112 5
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 179791 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 179791 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 69134 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 69134 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14339 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14339 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 14339 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 85691 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 85691 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 137265 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 137265 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14053 None 5 Human Functional pEC50 = 7.4 7.4 - 1
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 14053 None 5 Human Functional pEC50 = 7.4 7.4 - 1
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 14053 None 5 Human Functional pEC50 = 7.4 7.4 - 1
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 14098 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14098 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14098 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85949 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 85949 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 14064 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14064 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14064 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 85889 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 85889 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 138171 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 138171 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 164511 None 0 Human Functional pEC50 = 7.3 7.3 -33 2
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 164511 None 0 Human Functional pEC50 = 7.3 7.3 -33 2
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 164824 None 0 Human Functional pEC50 = 7.3 7.3 1 2
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 164824 None 0 Human Functional pEC50 = 7.3 7.3 1 2
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 216179 None 0 Rat Functional pEC50 = 8.3 8.3 3 2
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 216446 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
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 164780 None 0 Rat Functional pEC50 = 8.3 8.3 181 2
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 164780 None 0 Rat Functional pEC50 = 8.3 8.3 181 2
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 212765 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 182580 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 182580 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 71340 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 71340 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 14394 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14394 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14394 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 77358 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 77358 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 77358 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 14359 None 2 Human Functional pEC50 = 7.3 7.3 - 1
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 14359 None 2 Human Functional pEC50 = 7.3 7.3 - 1
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 14359 None 2 Human Functional pEC50 = 7.3 7.3 - 1
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 142120 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 142120 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14089 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14089 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14089 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14393 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 14393 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 14393 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 215483 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 163781 None 0 Human Functional pEC50 = 7.3 7.3 -14 2
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 163781 None 0 Human Functional pEC50 = 7.3 7.3 -14 2
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 14079 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14079 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 14079 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 85948 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 85948 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 14061 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14061 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14061 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14071 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14071 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14071 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 144705 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 144705 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 142123 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 142123 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 85701 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 85701 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 216633 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
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 210988 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
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 164196 None 0 Rat Functional pEC50 = 8.2 8.2 416 2
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 164196 None 0 Rat Functional pEC50 = 8.2 8.2 416 2
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 213522 None 7 Rat Functional pEC50 = 8.2 8.2 1 2
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 218322 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 182375 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 182375 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 164085 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 164085 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
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 85878 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 85878 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 164780 None 0 Human Functional pEC50 = 6.2 6.2 -181 2
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 164780 None 0 Human Functional pEC50 = 6.2 6.2 -181 2
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 135354 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 135354 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 14062 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14062 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14062 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14072 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14072 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14072 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14083 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 14083 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 14083 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 181094 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 181094 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 14055 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14055 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14055 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 164196 None 0 Human Functional pEC50 = 6.2 6.2 -416 2
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 164196 None 0 Human Functional pEC50 = 6.2 6.2 -416 2
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 14379 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14379 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14379 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14404 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14404 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 14404 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 163831 None 0 Human Functional pEC50 = 8.2 8.2 -1 2
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 163831 None 0 Human Functional pEC50 = 8.2 8.2 -1 2
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 164085 None 0 Rat Functional pEC50 = 8.1 8.1 1 2
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 164085 None 0 Rat Functional pEC50 = 8.1 8.1 1 2
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 217630 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
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 14387 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14387 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14387 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14060 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14060 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14060 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 181292 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 181292 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14054 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14054 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14054 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 218325 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14056 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14056 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 14056 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 164481 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 164481 None 0 Human Functional pEC50 = 6.1 6.1 -2 2
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 1647 None 23 Human Functional pEC50 = 7.1 7.1 - 1
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 1647 None 23 Human Functional pEC50 = 7.1 7.1 - 1
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 1647 None 23 Human Functional pEC50 = 7.1 7.1 - 1
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 181024 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 181024 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 218302 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 14050 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14050 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14050 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14078 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14078 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 14078 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 76746 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 76746 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 76746 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 85679 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 85679 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 163781 None 0 Human Functional pEC50 = 7.1 7.1 -14 2
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 163781 None 0 Human Functional pEC50 = 7.1 7.1 -14 2
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 218066 None 0 Rat Functional pEC50 = 8.0 8.0 - 1
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 182804 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 182804 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 213522 None 7 Human Functional pEC50 = 7.0 7.0 -1 2
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 181953 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 181953 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 14376 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14376 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14376 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14413 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14413 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 14413 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 2141 None 6 Rat Functional pIC50 = 9 9.0 7 2
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 2141 None 6 Rat Functional pIC50 = 9 9.0 7 2
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 2141 None 6 Rat Functional pIC50 = 9 9.0 7 2
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 199340 None 0 Rat Functional pIC50 = 9 9.0 501 2
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 199340 None 0 Rat Functional pIC50 = 9 9.0 501 2
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 151811 None 0 Rat Functional pIC50 = 8 8.0 - 1
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 151811 None 0 Rat Functional pIC50 = 8 8.0 - 1
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 171467 None 0 Human Functional pIC50 = 7 7.0 - 1
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 171467 None 0 Human Functional pIC50 = 7 7.0 - 1
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 91783 None 0 Rat Functional pIC50 = 7 7.0 - 1
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 91783 None 0 Rat Functional pIC50 = 7 7.0 - 1
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 88368 None 0 Human Functional pIC50 = 7 7.0 - 1
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 88368 None 0 Human Functional pIC50 = 7 7.0 - 1
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 199393 None 0 Rat Functional pIC50 = 6 6.0 - 1
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 199393 None 0 Rat Functional pIC50 = 6 6.0 - 1
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 199225 None 0 Rat Functional pIC50 = 8.0 8.0 3 2
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 199225 None 0 Rat Functional pIC50 = 8.0 8.0 3 2
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 199581 None 0 Rat Functional pIC50 = 8.0 8.0 4 2
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 199581 None 0 Rat Functional pIC50 = 8.0 8.0 4 2
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 199764 None 0 Rat Functional pIC50 = 8.0 8.0 69 2
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 199764 None 0 Rat Functional pIC50 = 8.0 8.0 69 2
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 171170 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 171170 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 173399 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 173399 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 174158 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 174158 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 199637 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 199637 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 199890 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 199890 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
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 88362 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 88362 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 174839 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 174839 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 175717 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 175717 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 199426 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 199426 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 199601 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 199601 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 88369 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 88369 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 201016 None 0 Human Functional pIC50 = 5.9 5.9 -93 2
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 201016 None 0 Human Functional pIC50 = 5.9 5.9 -93 2
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 88828 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
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 88828 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
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 171705 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 171705 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 201016 None 0 Rat Functional pIC50 = 7.9 7.9 93 2
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 201016 None 0 Rat Functional pIC50 = 7.9 7.9 93 2
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 174247 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 174247 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 175780 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 175780 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 200933 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 200933 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
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 199294 None 0 Human Functional pIC50 = 6.9 6.9 -6 2
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 199294 None 0 Human Functional pIC50 = 6.9 6.9 -6 2
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 201017 None 0 Human Functional pIC50 = 6.9 6.9 -8 2
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 201017 None 0 Human Functional pIC50 = 6.9 6.9 -8 2
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 88356 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 88356 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 88352 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 88352 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 199226 None 0 Rat Functional pIC50 = 7.9 7.9 15 2
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 199226 None 0 Rat Functional pIC50 = 7.9 7.9 15 2
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 199457 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
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 199457 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
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 3535 None 23 Human Functional pIC50 = 7.9 7.9 3 2
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 3535 None 23 Human Functional pIC50 = 7.9 7.9 3 2
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 3535 None 23 Human Functional pIC50 = 7.9 7.9 3 2
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 199940 None 0 Rat Functional pIC50 = 6.9 6.9 5 2
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 199940 None 0 Rat Functional pIC50 = 6.9 6.9 5 2
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 199478 None 0 Human Functional pIC50 = 6.9 6.9 -19 2
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 199478 None 0 Human Functional pIC50 = 6.9 6.9 -19 2
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 88363 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 88363 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 88353 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 88353 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 174251 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 174251 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 199360 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 199360 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 200213 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 200213 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 199407 None 0 Human Functional pIC50 = 6.8 6.8 -31 2
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 199407 None 0 Human Functional pIC50 = 6.8 6.8 -31 2
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 199578 None 0 Human Functional pIC50 = 6.8 6.8 -43 2
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 199578 None 0 Human Functional pIC50 = 6.8 6.8 -43 2
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 199620 None 0 Rat Functional pIC50 = 7.8 7.8 13 2
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 199620 None 0 Rat Functional pIC50 = 7.8 7.8 13 2
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 200148 None 0 Rat Functional pIC50 = 7.8 7.8 21 2
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 200148 None 0 Rat Functional pIC50 = 7.8 7.8 21 2
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 201017 None 0 Rat Functional pIC50 = 7.8 7.8 8 2
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 201017 None 0 Rat Functional pIC50 = 7.8 7.8 8 2
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 171206 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 171206 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 2995 None 41 Rat Functional pIC50 = 7.8 7.8 2 2
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 2995 None 41 Rat Functional pIC50 = 7.8 7.8 2 2
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 2995 None 41 Rat Functional pIC50 = 7.8 7.8 2 2
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 3526 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 3526 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 3526 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 199704 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
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 199704 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
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 199313 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 199313 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
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 88359 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 88359 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 91829 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
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 91829 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
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 200268 None 0 Human Functional pIC50 = 5.7 5.7 -22 2
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 200268 None 0 Human Functional pIC50 = 5.7 5.7 -22 2
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 88357 None 0 Human Functional pIC50 = 6.7 6.7 19 2
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 88357 None 0 Human Functional pIC50 = 6.7 6.7 19 2
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 201015 None 0 Rat Functional pIC50 = 8.7 8.7 251 2
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 201015 None 0 Rat Functional pIC50 = 8.7 8.7 251 2
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 199294 None 0 Rat Functional pIC50 = 7.7 7.7 6 2
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 199294 None 0 Rat Functional pIC50 = 7.7 7.7 6 2
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 199889 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 199889 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 201375 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 201375 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 88348 None 0 Rat Functional pIC50 = 5.7 5.7 -43 2
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 88348 None 0 Rat Functional pIC50 = 5.7 5.7 -43 2
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 88366 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 88366 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 90854 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 90854 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
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 199226 None 0 Human Functional pIC50 = 6.7 6.7 -15 2
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 199226 None 0 Human Functional pIC50 = 6.7 6.7 -15 2
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 199620 None 0 Human Functional pIC50 = 6.7 6.7 -13 2
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 199620 None 0 Human Functional pIC50 = 6.7 6.7 -13 2
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 201019 None 0 Rat Functional pIC50 = 7.6 7.6 2 2
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 201019 None 0 Rat Functional pIC50 = 7.6 7.6 2 2
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 170694 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 170694 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 171489 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 171489 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 199660 None 0 Human Functional pIC50 = 6.6 6.6 -8 2
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 199660 None 0 Human Functional pIC50 = 6.6 6.6 -8 2
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 89926 None 0 Rat Functional pIC50 = 4.6 4.6 - 1
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 89926 None 0 Rat Functional pIC50 = 4.6 4.6 - 1
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 199690 None 0 Human Functional pIC50 = 6.6 6.6 -3 2
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 199690 None 0 Human Functional pIC50 = 6.6 6.6 -3 2
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 146481 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 146481 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
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 172594 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 172594 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 173554 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 173554 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 199254 None 0 Human Functional pIC50 = 6.6 6.6 -3 2
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 199254 None 0 Human Functional pIC50 = 6.6 6.6 -3 2
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 169768 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 169768 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 199660 None 0 Rat Functional pIC50 = 7.5 7.5 8 2
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 199660 None 0 Rat Functional pIC50 = 7.5 7.5 8 2
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 199743 None 0 Rat Functional pIC50 = 8.5 8.5 17 2
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 199743 None 0 Rat Functional pIC50 = 8.5 8.5 17 2
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 199578 None 0 Rat Functional pIC50 = 8.5 8.5 43 2
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 199578 None 0 Rat Functional pIC50 = 8.5 8.5 43 2
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 199348 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 199348 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 88361 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 88361 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 171544 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 171544 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 2995 None 41 Human Functional pIC50 = 6.5 6.5 -2 2
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 2995 None 41 Human Functional pIC50 = 6.5 6.5 -2 2
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 2995 None 41 Human Functional pIC50 = 6.5 6.5 -2 2
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 201018 None 0 Human Functional pIC50 = 6.5 6.5 -52 2
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 201018 None 0 Human Functional pIC50 = 6.5 6.5 -52 2
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 172180 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 172180 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 89928 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 89928 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
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 3535 None 23 Rat Functional pIC50 = 7.5 7.5 -3 2
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 3535 None 23 Rat Functional pIC50 = 7.5 7.5 -3 2
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 3535 None 23 Rat Functional pIC50 = 7.5 7.5 -3 2
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 200148 None 0 Human Functional pIC50 = 6.5 6.5 -21 2
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 200148 None 0 Human Functional pIC50 = 6.5 6.5 -21 2
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 88373 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 88373 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 199225 None 0 Human Functional pIC50 = 7.4 7.4 -3 2
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 199225 None 0 Human Functional pIC50 = 7.4 7.4 -3 2
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 173359 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 173359 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 199229 None 0 Rat Functional pIC50 = 7.4 7.4 10 2
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 199229 None 0 Rat Functional pIC50 = 7.4 7.4 10 2
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 2995 None 41 Human Functional pIC50 = 7.4 7.4 -2 2
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 2995 None 41 Human Functional pIC50 = 7.4 7.4 -2 2
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 2995 None 41 Human Functional pIC50 = 7.4 7.4 -2 2
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 88357 None 0 Rat Functional pIC50 = 5.4 5.4 -19 2
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 88357 None 0 Rat Functional pIC50 = 5.4 5.4 -19 2
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 1010 None 6 Human Functional pIC50 = 8.4 8.4 - 1
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 1010 None 6 Human Functional pIC50 = 8.4 8.4 - 1
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 1010 None 6 Human Functional pIC50 = 8.4 8.4 - 1
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 200194 None 0 Rat Functional pIC50 = 8.4 8.4 128 2
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 200194 None 0 Rat Functional pIC50 = 8.4 8.4 128 2
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 200206 None 0 Rat Functional pIC50 = 8.4 8.4 15 2
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 200206 None 0 Rat Functional pIC50 = 8.4 8.4 15 2
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 199407 None 0 Rat Functional pIC50 = 8.3 8.3 31 2
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 199407 None 0 Rat Functional pIC50 = 8.3 8.3 31 2
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 199394 None 0 Rat Functional pIC50 = 7.4 7.4 12 2
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 199394 None 0 Rat Functional pIC50 = 7.4 7.4 12 2
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 145438 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
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 145438 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
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 199229 None 0 Human Functional pIC50 = 6.4 6.4 -10 2
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 199229 None 0 Human Functional pIC50 = 6.4 6.4 -10 2
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 88347 None 34 Human Functional pIC50 = 7.4 7.4 - 1
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 88347 None 34 Human Functional pIC50 = 7.4 7.4 - 1
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 89927 None 0 Rat Functional pIC50 = 4.4 4.4 - 1
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 89927 None 0 Rat Functional pIC50 = 4.4 4.4 - 1
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 199349 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
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 199349 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
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 199581 None 0 Human Functional pIC50 = 7.3 7.3 -4 2
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 199581 None 0 Human Functional pIC50 = 7.3 7.3 -4 2
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 170609 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 170609 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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
142747238 175638 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 175638 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 199340 None 0 Human Functional pIC50 = 6.3 6.3 -501 2
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 199340 None 0 Human Functional pIC50 = 6.3 6.3 -501 2
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 199394 None 0 Human Functional pIC50 = 6.3 6.3 -12 2
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 199394 None 0 Human Functional pIC50 = 6.3 6.3 -12 2
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 201015 None 0 Human Functional pIC50 = 6.3 6.3 -251 2
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 201015 None 0 Human Functional pIC50 = 6.3 6.3 -251 2
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 188077 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 188077 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 201019 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
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 201019 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
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 200194 None 0 Human Functional pIC50 = 6.3 6.3 -128 2
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 200194 None 0 Human Functional pIC50 = 6.3 6.3 -128 2
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 145442 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
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 145442 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
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 90918 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
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 90918 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
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 199743 None 0 Human Functional pIC50 = 7.3 7.3 -17 2
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 199743 None 0 Human Functional pIC50 = 7.3 7.3 -17 2
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 88365 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 88365 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 88370 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 88370 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 199647 None 0 Human Functional pIC50 = 7.2 7.2 -9 2
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 199647 None 0 Human Functional pIC50 = 7.2 7.2 -9 2
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 199647 None 0 Rat Functional pIC50 = 8.2 8.2 9 2
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 199647 None 0 Rat Functional pIC50 = 8.2 8.2 9 2
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 201018 None 0 Rat Functional pIC50 = 8.2 8.2 52 2
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 201018 None 0 Rat Functional pIC50 = 8.2 8.2 52 2
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 88348 None 0 Human Functional pIC50 = 7.2 7.2 43 2
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 88348 None 0 Human Functional pIC50 = 7.2 7.2 43 2
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 89988 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 89988 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
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 88367 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 88367 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 88358 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 88358 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 200206 None 0 Human Functional pIC50 = 7.2 7.2 -15 2
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 200206 None 0 Human Functional pIC50 = 7.2 7.2 -15 2
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 67663 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 67663 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 94951 None 1 Human Functional pIC50 = 6.2 6.2 -208 2
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 94951 None 1 Human Functional pIC50 = 6.2 6.2 -208 2
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
45486916 199699 None 0 Rat Functional pIC50 = 4.2 4.2 - 1
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 199699 None 0 Rat Functional pIC50 = 4.2 4.2 - 1
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 199254 None 0 Rat Functional pIC50 = 7.2 7.2 3 2
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 199254 None 0 Rat Functional pIC50 = 7.2 7.2 3 2
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 199478 None 0 Rat Functional pIC50 = 8.2 8.2 19 2
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 199478 None 0 Rat Functional pIC50 = 8.2 8.2 19 2
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 200193 None 0 Rat Functional pIC50 = 8.2 8.2 12 2
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 200193 None 0 Rat Functional pIC50 = 8.2 8.2 12 2
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 170003 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 170003 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 174612 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 174612 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 199400 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 199400 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
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 89284 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
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 89284 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
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 88349 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 88349 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 199832 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
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 199832 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
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 199764 None 0 Human Functional pIC50 = 6.1 6.1 -69 2
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 199764 None 0 Human Functional pIC50 = 6.1 6.1 -69 2
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 88360 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 88360 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 2141 None 6 Human Functional pIC50 = 8.1 8.1 -7 2
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 2141 None 6 Human Functional pIC50 = 8.1 8.1 -7 2
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 2141 None 6 Human Functional pIC50 = 8.1 8.1 -7 2
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 3535 None 23 Human Functional pIC50 = 8.1 8.1 3 2
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 3535 None 23 Human Functional pIC50 = 8.1 8.1 3 2
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 3535 None 23 Human Functional pIC50 = 8.1 8.1 3 2
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 169749 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 169749 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 170638 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 170638 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 175069 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 175069 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 199690 None 0 Rat Functional pIC50 = 7.1 7.1 3 2
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 199690 None 0 Rat Functional pIC50 = 7.1 7.1 3 2
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 199940 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
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 199940 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
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 200268 None 0 Rat Functional pIC50 = 7.1 7.1 22 2
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 200268 None 0 Rat Functional pIC50 = 7.1 7.1 22 2
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 200193 None 0 Human Functional pIC50 = 7.1 7.1 -12 2
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 200193 None 0 Human Functional pIC50 = 7.1 7.1 -12 2
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 169780 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 169780 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 173918 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 173918 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 176055 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 176055 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 146453 None 0 Rat Functional pIC50 = 5.0 5.0 - 1
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 146453 None 0 Rat Functional pIC50 = 5.0 5.0 - 1
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 88364 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 88364 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 155598 None 0 Human Functional pKd = 8 8.0 - 0
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 155598 None 0 Human Functional pKd = 8 8.0 - 0
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 214873 None 0 Rat Functional pKd = 8 8.0 - 0
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 188077 None 0 Human Functional pKd = 7 7.0 - 1
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 188077 None 0 Human Functional pKd = 7 7.0 - 1
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 193329 None 0 Human Functional pKd = 7 7.0 - 0
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 193329 None 0 Human Functional pKd = 7 7.0 - 0
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 188124 None 0 Human Functional pKd = 6.9 6.9 - 0
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 188124 None 0 Human Functional pKd = 6.9 6.9 - 0
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 187990 None 0 Human Functional pKd = 6.8 6.8 - 0
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 187990 None 0 Human Functional pKd = 6.8 6.8 - 0
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 188445 None 0 Human Functional pKd = 7.7 7.7 - 0
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 188445 None 0 Human Functional pKd = 7.7 7.7 - 0
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 214891 None 0 Rat Functional pKd = 7.4 7.4 - 0
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 211905 None 12 Rat Functional pKd = 8.3 8.3 - 0
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 214892 None 0 Rat Functional pKd = 7.3 7.3 - 0
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 211857 None 0 Rat Functional pKd = 6.1 6.1 - 0
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 3526 None 17 Human Functional pKi = 6.6 6.6 - 1
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 3526 None 17 Human Functional pKi = 6.6 6.6 - 1
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 3526 None 17 Human Functional pKi = 6.6 6.6 - 1
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 10481 None 0 Rat Functional pKi = 7.5 7.5 - 0
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 10481 None 0 Rat Functional pKi = 7.5 7.5 - 0
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 199457 None 0 Human Functional pKi = 6.4 6.4 - 1
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 199457 None 0 Human Functional pKi = 6.4 6.4 - 1
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 199457 None 0 Rat Functional pKi = 8.2 8.2 - 1
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 199457 None 0 Rat Functional pKi = 8.2 8.2 - 1
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 10466 None 0 Rat Functional pKi = 6.2 6.2 - 0
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 10466 None 0 Rat Functional pKi = 6.2 6.2 - 0
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 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
11663047 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
3501 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
3501 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
CHEMBL204989 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
CHEMBL204989 1647 None 23 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
9441 3956 None 0 Human Functional pEC50 = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27791374
9436 103 None 0 Human Functional pEC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12943190
2163 3452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
9803617 3452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
CHEMBL93758 3452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
10173280 2995 None 41 Human Functional pIC50 = 7.1 7.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
3516 2995 None 41 Human Functional pIC50 = 7.1 7.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
CHEMBL567303 2995 None 41 Human Functional pIC50 = 7.1 7.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
10886 3663 None 0 Human Functional pIC50 = 8 8.0 - 1
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 3663 None 0 Human Functional pIC50 = 8 8.0 - 1
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 3663 None 0 Human Functional pIC50 = 8 8.0 - 1
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 1486 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 1486 None 0 Human Functional pIC50 = 9.1 9.1 - 1
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 3961 None 0 Human Functional pIC50 None 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
2156 3961 None 0 Human Functional pIC50 None 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
CHEMBL437110 3961 None 0 Human Functional pIC50 None 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL3315148 213831 None 0 Rat Binding pEC50 = 10.9 10.9 - 1
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 213827 None 0 Rat Binding pEC50 = 10.7 10.7 - 1
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 213822 None 10 Rat Binding pEC50 = 9.4 9.4 - 1
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 213835 None 0 Rat Binding pEC50 = 9.2 9.2 - 1
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 213823 None 0 Rat Binding pEC50 = 9.1 9.1 - 1
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 213829 None 0 Rat Binding pEC50 = 9.1 9.1 - 1
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 216179 None 0 Rat Binding pEC50 = 9.1 9.1 - 1
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 216179 None 0 Rat Binding pEC50 = 9 9.0 - 1
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 213833 None 0 Rat Binding pEC50 = 9.0 9.0 - 1
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 161090 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
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 161090 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
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 161090 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
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 121271 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 121271 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 121271 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 121271 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 141115 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 141115 None 0 Rat Binding pEC50 = 8.8 8.8 - 0
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 211862 None 0 Human Binding pEC50 = 8.7 8.7 - 1
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 161198 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 161198 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 161198 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 161226 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 161226 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 161226 None 0 Rat Binding pEC50 = 8 8.0 - 0
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 121269 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121269 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161274 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161274 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161274 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121269 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121269 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161286 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 161286 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 161286 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 161275 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161275 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161275 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 161260 None 0 Human Binding pEC50 = 8.0 8.0 - 0
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 75964 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 75964 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 170478 None 0 Human Binding pEC50 = 7.0 7.0 - 1
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 170478 None 0 Human Binding pEC50 = 7.0 7.0 - 1
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 77374 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 77374 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 141446 None 0 Human Binding pEC50 = 7.0 7.0 - 0
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 141446 None 0 Human Binding pEC50 = 7.0 7.0 - 0
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 161260 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 161260 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 161260 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 121261 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121261 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161249 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161249 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161249 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121261 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121261 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121263 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121263 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121263 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121263 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 244 None 10 Human Binding pEC50 = 6.0 6.0 - 1
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 244 None 10 Human Binding pEC50 = 6.0 6.0 - 1
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 244 None 10 Human Binding pEC50 = 6.0 6.0 - 1
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 77389 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 77389 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 98313 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 98313 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 77387 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 77387 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 213518 None 0 Rat Binding pEC50 = 6.9 6.9 - 0
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 166131 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 166131 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 213518 None 0 Rat Binding pEC50 = 6.9 6.9 - 0
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 161296 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 161296 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 161296 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 161260 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 161260 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 161260 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 161255 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161255 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161255 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121260 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121260 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121260 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 121260 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 213832 None 0 Rat Binding pEC50 = 7.9 7.9 - 1
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 198052 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 198052 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 161236 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161236 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161236 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 141026 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 141026 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 173419 None 0 Human Binding pEC50 = 7.9 7.9 - 1
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 173419 None 0 Human Binding pEC50 = 7.9 7.9 - 1
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 161285 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161285 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 161285 None 0 Rat Binding pEC50 = 7.9 7.9 - 0
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 140254 None 7 Human Binding pEC50 = 6.9 6.9 - 0
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 140254 None 7 Human Binding pEC50 = 6.9 6.9 - 0
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 74791 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 74791 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 75081 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 75081 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 75987 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 75987 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 138793 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 138793 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 161296 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 161296 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 161296 None 0 Human Binding pEC50 = 7.8 7.8 - 0
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 75035 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 75035 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 76792 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 76792 None 0 Human Binding pEC50 = 6.8 6.8 - 0
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 74781 None 1 Human Binding pEC50 = 5.8 5.8 - 0
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 74781 None 1 Human Binding pEC50 = 5.8 5.8 - 0
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 74781 None 1 Human Binding pEC50 = 5.8 5.8 - 0
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 161285 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161285 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161285 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 141048 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 141048 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161068 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161068 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161068 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 75584 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 75584 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76009 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76009 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 213516 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
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 161296 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161296 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161296 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161226 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161226 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 161226 None 0 Rat Binding pEC50 = 7.8 7.8 - 0
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 213516 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
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 140435 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 140435 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 77203 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 77203 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76307 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76307 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76655 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 76655 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 161295 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 161295 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 161295 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 140804 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 140804 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 213826 None 0 Rat Binding pEC50 = 7.7 7.7 - 1
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 159036 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 159036 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 175185 None 0 Human Binding pEC50 = 7.7 7.7 - 1
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 175185 None 0 Human Binding pEC50 = 7.7 7.7 - 1
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 213515 None 0 Rat Binding pEC50 = 6.7 6.7 - 0
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 138800 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 138800 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 75501 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 75501 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 121270 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121270 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121270 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121270 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161255 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161255 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161255 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161320 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161320 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 161320 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 141385 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 141385 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 76755 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76755 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 138977 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 138977 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161286 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161286 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161286 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 171843 None 0 Rat Binding pEC50 = 6.7 6.7 - 1
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 171843 None 0 Rat Binding pEC50 = 6.7 6.7 - 1
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 244 None 10 Rat Binding pEC50 = 6.7 6.7 - 1
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 244 None 10 Rat Binding pEC50 = 6.7 6.7 - 1
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 244 None 10 Rat Binding pEC50 = 6.7 6.7 - 1
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 76080 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76080 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 141151 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 141151 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 141085 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 141085 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 121261 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 121261 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 213830 None 0 Rat Binding pEC50 = 8.6 8.6 - 1
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 172359 None 0 Human Binding pEC50 = 8.6 8.6 - 1
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 172359 None 0 Human Binding pEC50 = 8.6 8.6 - 1
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 213522 None 7 Human Binding pEC50 = 8.6 8.6 - 1
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 121261 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 121261 None 0 Rat Binding pEC50 = 8.6 8.6 - 0
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 213520 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 76765 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76765 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 213520 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121265 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121265 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121265 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 121265 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 213519 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 76054 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76054 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76756 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76756 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 77690 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 77690 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161296 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161296 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161296 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 213519 None 0 Rat Binding pEC50 = 7.7 7.7 - 0
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 171843 None 0 Human Binding pEC50 = 7.7 7.7 - 1
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 171843 None 0 Human Binding pEC50 = 7.7 7.7 - 1
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 161295 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161295 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 161295 None 0 Human Binding pEC50 = 5.7 5.7 - 0
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 76005 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 76005 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 76775 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 76775 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 121260 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 121260 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 121260 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 121260 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 172359 None 0 Rat Binding pEC50 = 7.6 7.6 - 1
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 172359 None 0 Rat Binding pEC50 = 7.6 7.6 - 1
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 159036 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 159036 None 0 Rat Binding pEC50 = 7.6 7.6 - 0
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 213517 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
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 74726 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 74726 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 213517 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
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 244 None 10 Human Binding pEC50 = 6.6 6.6 - 1
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 244 None 10 Human Binding pEC50 = 6.6 6.6 - 1
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 244 None 10 Human Binding pEC50 = 6.6 6.6 - 1
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 75560 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 75560 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 213521 None 0 Rat Binding pEC50 = 6.6 6.6 - 0
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 75079 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 75079 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 76058 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 76058 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 141374 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 141374 None 0 Human Binding pEC50 = 5.6 5.6 - 0
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 76745 None 0 Human Binding pEC50 = 6.5 6.5 - 0
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 76745 None 0 Human Binding pEC50 = 6.5 6.5 - 0
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 141122 None 0 Human Binding pEC50 = 5.5 5.5 - 0
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 141122 None 0 Human Binding pEC50 = 5.5 5.5 - 0
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 218303 None 7 Human Binding pEC50 = 8.5 8.5 - 1
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 218303 None 7 Rat Binding pEC50 = 8.5 8.5 - 1
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 218303 None 7 Rat Binding pEC50 = 8.5 8.5 - 1
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 161106 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161106 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161106 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161236 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161236 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161236 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161286 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161286 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161286 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161295 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161295 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161295 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 175169 None 0 Rat Binding pEC50 = 8.5 8.5 - 1
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 175169 None 0 Rat Binding pEC50 = 8.5 8.5 - 1
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 161320 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161320 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161320 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 121270 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 121270 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 121270 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 121270 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 161169 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 141035 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 141035 None 0 Rat Binding pEC50 = 8.5 8.5 - 0
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 211862 None 0 Rat Binding pEC50 = 8.4 8.4 - 1
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 175169 None 0 Human Binding pEC50 = 8.4 8.4 - 1
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 175169 None 0 Human Binding pEC50 = 8.4 8.4 - 1
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 161193 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161193 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161193 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121267 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121267 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121267 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121267 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161090 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161090 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161090 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161249 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161249 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161249 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161115 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161115 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161115 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161198 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161198 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161198 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 141115 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 141115 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 213824 None 0 Rat Binding pEC50 = 8.4 8.4 - 1
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 161142 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161142 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161142 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161286 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161286 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161286 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161163 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161163 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161163 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 244 None 10 Human Binding pEC50 = 6.5 6.5 - 1
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 244 None 10 Human Binding pEC50 = 6.5 6.5 - 1
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 244 None 10 Human Binding pEC50 = 6.5 6.5 - 1
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 77185 None 0 Human Binding pEC50 = 7.5 7.5 - 0
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 77185 None 0 Human Binding pEC50 = 7.5 7.5 - 0
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 77185 None 0 Human Binding pEC50 = 7.5 7.5 - 0
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 213828 None 0 Rat Binding pEC50 = 7.5 7.5 - 1
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 74467 None 0 Human Binding pEC50 = 5.5 5.5 - 0
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 74467 None 0 Human Binding pEC50 = 5.5 5.5 - 0
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 75977 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 75977 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 161286 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 161286 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 161286 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 213515 None 0 Rat Binding pEC50 = 6.4 6.4 - 0
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 76025 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 76025 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 121265 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121265 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161078 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161078 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161078 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161205 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161205 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161205 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161296 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 161296 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 161296 None 0 Human Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161250 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121266 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121266 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121266 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121266 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161260 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161260 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161260 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 176141 None 0 Rat Binding pEC50 = 8.4 8.4 - 1
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 176141 None 0 Rat Binding pEC50 = 8.4 8.4 - 1
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 161275 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161275 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 161275 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121270 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121270 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121270 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121270 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121268 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121268 None 0 Rat Binding pEC50 = 8.4 8.4 - 0
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 121268 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121268 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 170996 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 170996 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 121265 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121265 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161067 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161067 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161067 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 141035 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 141035 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121267 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121267 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121267 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121267 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 172229 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 172229 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 161078 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161078 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161078 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121272 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121272 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 213528 None 0 Rat Binding pEC50 = 7.4 7.4 - 0
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 213528 None 0 Rat Binding pEC50 = 7.4 7.4 - 0
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 77176 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 77176 None 0 Human Binding pEC50 = 6.4 6.4 - 0
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 140426 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 140426 None 0 Human Binding pEC50 = 5.4 5.4 - 0
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 76800 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 76800 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 121272 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121272 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 213825 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 161260 None 0 Human Binding pEC50 = 8.3 8.3 - 0
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 161260 None 0 Human Binding pEC50 = 8.3 8.3 - 0
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 161260 None 0 Human Binding pEC50 = 8.3 8.3 - 0
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 161115 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161115 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161115 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161142 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161142 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161142 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161274 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161274 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161274 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 141080 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 141080 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 171535 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 171535 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 170996 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 170996 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 211862 None 0 Rat Binding pEC50 = 8.3 8.3 - 1
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 161287 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121264 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121264 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121264 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121264 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 172449 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 172449 None 0 Human Binding pEC50 = 8.3 8.3 - 1
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 121268 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121268 None 0 Rat Binding pEC50 = 8.3 8.3 - 0
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 121268 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121268 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 172449 None 0 Rat Binding pEC50 = 8.2 8.2 - 1
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 172449 None 0 Rat Binding pEC50 = 8.2 8.2 - 1
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 161067 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161067 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161067 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 77358 None 0 Human Binding pEC50 = 5.3 5.3 - 0
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 77358 None 0 Human Binding pEC50 = 5.3 5.3 - 0
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 77358 None 0 Human Binding pEC50 = 5.3 5.3 - 0
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 213525 None 0 Rat Binding pEC50 = 6.3 6.3 - 0
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 141184 None 0 Human Binding pEC50 = 5.3 5.3 - 0
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 141184 None 0 Human Binding pEC50 = 5.3 5.3 - 0
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 75420 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 75420 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 76541 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 76541 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 213523 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
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 175185 None 0 Rat Binding pEC50 = 6.3 6.3 - 1
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 175185 None 0 Rat Binding pEC50 = 6.3 6.3 - 1
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 213523 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
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 161068 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161068 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161068 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161286 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 161286 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 161286 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 161163 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161163 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161163 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161295 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161295 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161295 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121263 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121263 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121263 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121263 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161205 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161205 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 161205 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121262 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121262 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121262 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 121262 None 0 Rat Binding pEC50 = 8.2 8.2 - 0
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 138791 None 0 Human Binding pEC50 = 5.2 5.2 - 0
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 138791 None 0 Human Binding pEC50 = 5.2 5.2 - 0
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 75177 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 75177 None 0 Human Binding pEC50 = 7.2 7.2 - 0
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 213522 None 7 Rat Binding pEC50 = 8.2 8.2 - 1
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 161295 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 161295 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 161295 None 0 Human Binding pEC50 = 8.2 8.2 - 0
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 213522 None 7 Rat Binding pEC50 = 8.1 8.1 - 1
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 161106 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 161106 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 161106 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121264 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121264 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121264 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121264 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 141080 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 141080 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 1647 None 23 Human Binding pEC50 = 7.1 7.1 - 0
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 1647 None 23 Human Binding pEC50 = 7.1 7.1 - 0
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 1647 None 23 Human Binding pEC50 = 7.1 7.1 - 0
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 75943 None 0 Human Binding pEC50 = 7.1 7.1 - 0
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 75943 None 0 Human Binding pEC50 = 7.1 7.1 - 0
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 121266 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121266 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 213522 None 7 Rat Binding pEC50 = 8.1 8.1 - 1
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 121266 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121266 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121272 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121272 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121272 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121272 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 161295 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 161295 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 161295 None 0 Human Binding pEC50 = 8.1 8.1 - 0
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 161193 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 161193 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 161193 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121271 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121271 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121269 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121269 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121271 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121271 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121269 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 121269 None 0 Rat Binding pEC50 = 8.1 8.1 - 0
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 213524 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
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 173419 None 0 Rat Binding pEC50 = 7.1 7.1 - 1
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 173419 None 0 Rat Binding pEC50 = 7.1 7.1 - 1
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 213521 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
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 213524 None 0 Rat Binding pEC50 = 6.1 6.1 - 0
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 76746 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 76746 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 76746 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 213525 None 0 Rat Binding pEC50 = 7.1 7.1 - 0
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 141085 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 141085 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161296 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161296 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 161296 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121262 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121262 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121262 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 121262 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 171535 None 0 Rat Binding pEC50 = 8.0 8.0 - 1
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 171535 None 0 Rat Binding pEC50 = 8.0 8.0 - 1
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 141048 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 141048 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 141026 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 141026 None 0 Rat Binding pEC50 = 8.0 8.0 - 0
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 170639 None 0 Rat Binding pEC50 = 8.0 8.0 - 1
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 170639 None 0 Rat Binding pEC50 = 8.0 8.0 - 1
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 181901 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 181901 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 213519 None 0 Human Binding pIC50 = 8 8.0 - 0
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 144558 None 0 Human Binding pIC50 = 7 7.0 - 0
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 144558 None 0 Human Binding pIC50 = 7 7.0 - 0
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 151025 None 0 Human Binding pIC50 = 7 7.0 - 0
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 151025 None 0 Human Binding pIC50 = 7 7.0 - 0
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 177546 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 177546 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 181006 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 181006 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 213522 None 7 Human Binding pIC50 = 7.9 7.9 - 1
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 177934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 177934 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 213522 None 7 Human Binding pIC50 = 7.9 7.9 - 1
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 174247 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 174247 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 151385 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 151385 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 88356 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 88356 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 116322 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 116322 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 88349 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 88349 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 216179 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 116330 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 116330 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 216179 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 153601 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 153601 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 88368 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 88368 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 177829 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 177829 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 88353 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 88353 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 171544 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 171544 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 143527 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 143527 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 144627 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 144627 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 116326 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 116326 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 169749 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 169749 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 171467 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 171467 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 175780 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 175780 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 176055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 176055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177301 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 177301 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 179961 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 179961 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 3526 None 17 Human Binding pIC50 = 6.8 6.8 -1 3
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 3526 None 17 Human Binding pIC50 = 6.8 6.8 -1 3
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 3526 None 17 Human Binding pIC50 = 6.8 6.8 -1 3
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 213523 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 88369 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 88369 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 116313 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 116313 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 182995 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 182995 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 213523 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 174251 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 174251 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 175717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 175717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 88367 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 88367 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 154373 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 154373 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 213526 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 213526 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 213522 None 7 Human Binding pIC50 = 7.7 7.7 - 1
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 116327 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 116327 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 179620 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 179620 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 177295 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 177295 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 174158 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 174158 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 116325 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 116325 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 116328 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 116328 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 213520 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 213520 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 88374 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 88374 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 116316 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 116316 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 88357 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 88357 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 116315 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 116315 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 88347 None 34 Human Binding pIC50 = 7.6 7.6 - 0
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 88347 None 34 Human Binding pIC50 = 7.6 7.6 - 0
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 88352 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 88352 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 170609 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 170609 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 173554 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 173554 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 88350 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 88350 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 153314 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 153314 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 170003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 170003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 116323 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 116323 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 164481 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 164481 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 174839 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 174839 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 175069 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 175069 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 213518 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 88366 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 88366 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 213527 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 213527 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 213517 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 213518 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 213517 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 177825 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 177825 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 2995 None 41 Human Binding pIC50 = 8.4 8.4 -3 6
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 2995 None 41 Human Binding pIC50 = 8.4 8.4 -3 6
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 2995 None 41 Human Binding pIC50 = 8.4 8.4 -3 6
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 163831 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 163831 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 181399 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 181399 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 181292 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 181292 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 88355 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 88355 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 174612 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 174612 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 150028 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 150028 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 116321 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 116321 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 175638 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 175638 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 171206 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 171206 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 88348 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 88348 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 152650 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 152650 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 88358 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 88358 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 116318 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 116318 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177178 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177178 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 213514 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 213514 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 172180 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 172180 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 171489 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 171489 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 116329 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 116329 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 169768 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 169768 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 181024 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 181024 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 88351 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 88351 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 88364 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 88364 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 116317 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 116317 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 213524 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 213524 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 169780 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 169780 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 170694 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 170694 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 183028 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 183028 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 183601 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 183601 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 152381 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 152381 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 153303 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 153303 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 213522 None 7 Human Binding pIC50 = 8.3 8.3 - 1
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 164085 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 164085 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 164824 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 164824 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 143336 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 143336 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 88360 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 88360 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 88365 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 88365 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 146884 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 146884 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 145713 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 145713 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 213525 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 213525 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 171170 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 171170 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 3535 None 23 Human Binding pIC50 = 8.2 8.2 2 3
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 3535 None 23 Human Binding pIC50 = 8.2 8.2 2 3
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 3535 None 23 Human Binding pIC50 = 8.2 8.2 2 3
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 171705 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 171705 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 213516 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 116324 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 116324 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 213516 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 180377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 180377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 116314 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 116314 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 172594 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 172594 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 146367 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 146367 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88363 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88363 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88371 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 88371 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 147085 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 147085 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 173359 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 173359 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 88354 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88354 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 10429 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 10429 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 173918 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 173918 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 88362 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88362 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 177512 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 177512 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 88361 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 88361 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 152321 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 152321 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 153375 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 153375 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 149057 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 149057 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 116320 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 116320 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 182753 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 182753 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 213528 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 143448 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 143448 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 88373 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 88373 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 213515 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 213515 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 88359 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 88359 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 88372 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 88372 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 145717 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 145717 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 154451 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 154451 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 213521 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 213521 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 179535 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 179535 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 173399 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 173399 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 213528 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 153478 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 153478 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 170638 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 170638 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 116319 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 116319 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 147945 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 147945 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 210993 None 0 Rat Binding pKi = 10.7 10.7 - 1
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 218267 None 0 Rat Binding pKi = 9.9 9.9 - 1
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 218267 None 0 Rat Binding pKi = 9.9 9.9 - 1
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 210978 None 6 Rat Binding pKi = 9.7 9.7 - 1
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 214897 None 0 Human Binding pKi = 9.7 9.7 - 1
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 214897 None 0 Human Binding pKi = 9.7 9.7 - 1
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 214897 None 0 Human Binding pKi = 9.7 9.7 - 1
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 214897 None 0 Human Binding pKi = 9.7 9.7 - 1
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 213822 None 10 Human Binding pKi = 9.7 9.7 - 1
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 215804 None 0 Human Binding pKi = 9.6 9.6 - 1
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 215804 None 0 Human Binding pKi = 9.6 9.6 - 1
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 215804 None 0 Human Binding pKi = 9.6 9.6 - 1
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 215804 None 0 Human Binding pKi = 9.6 9.6 - 1
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 211862 None 0 Human Binding pKi = 9.6 9.6 - 1
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 216662 None 0 Human Binding pKi = 9.6 9.6 - 1
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 173810 None 0 Human Binding pKi = 9.5 9.5 - 1
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 173810 None 0 Human Binding pKi = 9.5 9.5 - 1
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 213825 None 0 Human Binding pKi = 9.4 9.4 - 1
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 95166 None 0 Human Binding pKi = 9.4 9.4 - 1
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 95166 None 0 Human Binding pKi = 9.4 9.4 - 1
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 95516 None 0 Human Binding pKi = 9.4 9.4 - 1
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 95516 None 0 Human Binding pKi = 9.4 9.4 - 1
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 95469 None 0 Human Binding pKi = 9.2 9.2 - 1
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 95469 None 0 Human Binding pKi = 9.2 9.2 - 1
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 213824 None 0 Human Binding pKi = 9.1 9.1 - 1
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 213831 None 0 Human Binding pKi = 9.1 9.1 - 1
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 216179 None 0 Human Binding pKi = 9.1 9.1 - 1
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 216179 None 0 Human Binding pKi = 9.1 9.1 - 1
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 216179 None 0 Human Binding pKi = 9.1 9.1 - 1
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 216179 None 0 Human Binding pKi = 9.1 9.1 - 1
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 218066 None 0 Human Binding pKi = 9.1 9.1 - 1
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 218303 None 7 Human Binding pKi = 9.1 9.1 - 1
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 218075 None 0 Human Binding pKi = 9.1 9.1 - 1
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 212614 None 0 Human Binding pKi = 9.0 9.0 - 1
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 95571 None 0 Human Binding pKi = 9 9.0 - 1
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 95571 None 0 Human Binding pKi = 9 9.0 - 1
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 213830 None 0 Human Binding pKi = 9.0 9.0 - 1
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 214806 None 0 Human Binding pKi = 9.0 9.0 - 1
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 95156 None 0 Human Binding pKi = 8.9 8.9 - 1
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 95156 None 0 Human Binding pKi = 8.9 8.9 - 1
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 211862 None 0 Human Binding pKi = 8.9 8.9 - 1
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 213829 None 0 Human Binding pKi = 8.9 8.9 - 1
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 212391 None 0 Human Binding pKi = 8.9 8.9 - 1
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 212391 None 0 Human Binding pKi = 8.9 8.9 - 1
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 211908 None 0 Human Binding pKi = 8.9 8.9 - 1
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 214874 None 0 Human Binding pKi = 8.9 8.9 - 1
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 214661 None 0 Human Binding pKi = 8.8 8.8 - 1
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 216418 None 0 Human Binding pKi = 8.8 8.8 - 1
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 172229 None 0 Human Binding pKi = 8.8 8.8 - 1
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 172229 None 0 Human Binding pKi = 8.8 8.8 - 1
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 175169 None 0 Human Binding pKi = 8.8 8.8 - 1
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 175169 None 0 Human Binding pKi = 8.8 8.8 - 1
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 213827 None 0 Human Binding pKi = 8.8 8.8 - 1
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 213835 None 0 Human Binding pKi = 8.8 8.8 - 1
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 213833 None 0 Human Binding pKi = 8.7 8.7 - 1
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 213823 None 0 Human Binding pKi = 8.7 8.7 - 1
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 188125 None 0 Human Binding pKi = 8 8.0 - 1
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 188125 None 0 Human Binding pKi = 8 8.0 - 1
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 193329 None 0 Human Binding pKi = 8 8.0 39 2
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 193329 None 0 Human Binding pKi = 8 8.0 39 2
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 155598 None 0 Rat Binding pKi = 8 8.0 -1 2
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 155598 None 0 Rat Binding pKi = 8 8.0 -1 2
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 215434 None 0 Human Binding pKi = 8 8.0 - 1
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 214892 None 0 Human Binding pKi = 8 8.0 5 2
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 183640 None 0 Human Binding pKi = 8 8.0 - 1
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 183640 None 0 Human Binding pKi = 8 8.0 - 1
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 95424 None 0 Human Binding pKi = 7 7.0 - 1
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 95424 None 0 Human Binding pKi = 7 7.0 - 1
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 188107 None 0 Human Binding pKi = 7 7.0 - 1
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 188107 None 0 Human Binding pKi = 7 7.0 - 1
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 188162 None 0 Human Binding pKi = 7 7.0 - 1
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 188162 None 0 Human Binding pKi = 7 7.0 - 1
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 67657 None 0 Human Binding pKi = 6 6.0 - 1
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 67657 None 0 Human Binding pKi = 6 6.0 - 1
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 187990 None 0 Cat Binding pKi = 6 6.0 -15 2
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 187990 None 0 Cat Binding pKi = 6 6.0 -15 2
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 188445 None 0 Cat Binding pKi = 6 6.0 -63 2
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 188445 None 0 Cat Binding pKi = 6 6.0 -63 2
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 95561 None 0 Human Binding pKi = 6 6.0 - 1
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 95561 None 0 Human Binding pKi = 6 6.0 - 1
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 183955 None 0 Human Binding pKi = 6 6.0 - 1
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 183955 None 0 Human Binding pKi = 6 6.0 - 1
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 197253 None 0 Human Binding pKi = 7.0 7.0 - 1
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 197253 None 0 Human Binding pKi = 7.0 7.0 - 1
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 201015 None 0 Human Binding pKi = 8.0 8.0 - 1
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 201015 None 0 Human Binding pKi = 8.0 8.0 - 1
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 201017 None 0 Human Binding pKi = 8.0 8.0 - 1
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 201017 None 0 Human Binding pKi = 8.0 8.0 - 1
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 217752 None 0 Human Binding pKi = 7.9 7.9 - 1
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 67663 None 0 Human Binding pKi = 7.0 7.0 - 1
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 67663 None 0 Human Binding pKi = 7.0 7.0 - 1
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 210984 None 0 Rat Binding pKi = 6.0 6.0 - 1
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 10466 None 0 Human Binding pKi = 7.9 7.9 50 2
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 10466 None 0 Human Binding pKi = 7.9 7.9 50 2
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 188866 None 0 Human Binding pKi = 7.9 7.9 - 1
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 188866 None 0 Human Binding pKi = 7.9 7.9 - 1
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 213834 None 0 Human Binding pKi = 7.9 7.9 - 1
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 212392 None 0 Human Binding pKi = 7.9 7.9 - 1
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 212737 None 0 Human Binding pKi = 7.9 7.9 - 1
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 187909 None 0 Human Binding pKi = 7.9 7.9 - 1
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 187909 None 0 Human Binding pKi = 7.9 7.9 - 1
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 187916 None 0 Human Binding pKi = 7.9 7.9 125 2
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 187916 None 0 Human Binding pKi = 7.9 7.9 125 2
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 188445 None 0 Human Binding pKi = 7.9 7.9 63 2
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 188445 None 0 Human Binding pKi = 7.9 7.9 63 2
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 214873 None 0 Human Binding pKi = 7.9 7.9 -1 2
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 213828 None 0 Human Binding pKi = 7.9 7.9 - 1
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 199254 None 0 Human Binding pKi = 6.9 6.9 - 1
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 199254 None 0 Human Binding pKi = 6.9 6.9 - 1
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 190874 None 0 Human Binding pKi = 6.9 6.9 - 1
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 190874 None 0 Human Binding pKi = 6.9 6.9 - 1
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 3528 None 33 Rat Binding pKi = 6.9 6.9 2 2
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 3528 None 33 Rat Binding pKi = 6.9 6.9 2 2
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 3528 None 33 Rat Binding pKi = 6.9 6.9 2 2
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 67663 None 0 Human Binding pKi = 6.9 6.9 - 1
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 67663 None 0 Human Binding pKi = 6.9 6.9 - 1
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 68651 None 0 Human Binding pKi = 6.9 6.9 - 1
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 68651 None 0 Human Binding pKi = 6.9 6.9 - 1
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 193329 None 0 Cat Binding pKi = 5.9 5.9 -39 2
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 193329 None 0 Cat Binding pKi = 5.9 5.9 -39 2
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 171836 None 0 Human Binding pKi = 5.9 5.9 - 1
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 171836 None 0 Human Binding pKi = 5.9 5.9 - 1
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 173617 None 0 Human Binding pKi = 7.9 7.9 - 1
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 173617 None 0 Human Binding pKi = 7.9 7.9 - 1
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 186808 None 0 Human Binding pKi = 7.9 7.9 - 1
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 186808 None 0 Human Binding pKi = 7.9 7.9 - 1
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 199581 None 0 Human Binding pKi = 7.9 7.9 - 1
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 199581 None 0 Human Binding pKi = 7.9 7.9 - 1
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 217630 None 0 Human Binding pKi = 7.9 7.9 - 1
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 155350 None 0 Human Binding pKi = 6.9 6.9 - 1
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 155350 None 0 Human Binding pKi = 6.9 6.9 - 1
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 199764 None 0 Human Binding pKi = 6.9 6.9 - 1
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 199764 None 0 Human Binding pKi = 6.9 6.9 - 1
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 215665 None 0 Human Binding pKi = 6.9 6.9 - 1
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 89988 None 0 Human Binding pKi = 6.9 6.9 - 1
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 89988 None 0 Human Binding pKi = 6.9 6.9 - 1
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 184164 None 0 Human Binding pKi = 6.9 6.9 - 1
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 184164 None 0 Human Binding pKi = 6.9 6.9 - 1
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 199890 None 0 Human Binding pKi = 5.9 5.9 - 1
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 199890 None 0 Human Binding pKi = 5.9 5.9 - 1
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 193813 None 0 Human Binding pKi = 7.8 7.8 - 1
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 193813 None 0 Human Binding pKi = 7.8 7.8 - 1
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 210991 None 0 Rat Binding pKi = 7.8 7.8 - 1
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 201018 None 0 Human Binding pKi = 7.8 7.8 - 1
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 201018 None 0 Human Binding pKi = 7.8 7.8 - 1
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 192693 None 0 Human Binding pKi = 7.8 7.8 - 1
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 192693 None 0 Human Binding pKi = 7.8 7.8 - 1
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 95249 None 0 Human Binding pKi = 7.8 7.8 - 1
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 95249 None 0 Human Binding pKi = 7.8 7.8 - 1
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 155262 None 1 Human Binding pKi = 7.8 7.8 -1 2
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 155262 None 1 Human Binding pKi = 7.8 7.8 -1 2
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 214891 None 0 Human Binding pKi = 7.8 7.8 2 2
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 216617 None 0 Human Binding pKi = 7.8 7.8 - 1
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 199394 None 0 Human Binding pKi = 6.8 6.8 - 1
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 199394 None 0 Human Binding pKi = 6.8 6.8 - 1
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 184159 None 0 Human Binding pKi = 5.8 5.8 - 1
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 184159 None 0 Human Binding pKi = 5.8 5.8 - 1
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 172611 None 0 Human Binding pKi = 5.8 5.8 - 1
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 172611 None 0 Human Binding pKi = 5.8 5.8 - 1
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 215797 None 0 Human Binding pKi = 6.8 6.8 - 1
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 123419 None 0 Human Binding pKi = 6.8 6.8 - 1
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 123419 None 0 Human Binding pKi = 6.8 6.8 - 1
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 168858 None 0 Human Binding pKi = 6.8 6.8 - 1
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 168858 None 0 Human Binding pKi = 6.8 6.8 - 1
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 187916 None 0 Cat Binding pKi = 5.8 5.8 -125 2
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 187916 None 0 Cat Binding pKi = 5.8 5.8 -125 2
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 94950 None 1 Human Binding pKi = 5.8 5.8 - 1
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 94950 None 1 Human Binding pKi = 5.8 5.8 - 1
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 95299 None 0 Human Binding pKi = 5.8 5.8 - 1
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 95299 None 0 Human Binding pKi = 5.8 5.8 - 1
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 172531 None 0 Human Binding pKi = 5.8 5.8 - 1
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 172531 None 0 Human Binding pKi = 5.8 5.8 - 1
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 94987 None 1 Human Binding pKi = 7.8 7.8 - 1
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 94987 None 1 Human Binding pKi = 7.8 7.8 - 1
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 173618 None 0 Human Binding pKi = 7.8 7.8 - 1
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 173618 None 0 Human Binding pKi = 7.8 7.8 - 1
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 94987 None 1 Human Binding pKi = 7.8 7.8 - 1
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 94987 None 1 Human Binding pKi = 7.8 7.8 - 1
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 199226 None 0 Human Binding pKi = 7.8 7.8 - 1
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 199226 None 0 Human Binding pKi = 7.8 7.8 - 1
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 213836 None 0 Human Binding pKi = 7.8 7.8 - 1
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 145442 None 0 Human Binding pKi = 6.8 6.8 - 1
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 145442 None 0 Human Binding pKi = 6.8 6.8 - 1
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 199360 None 0 Human Binding pKi = 6.8 6.8 - 1
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 199360 None 0 Human Binding pKi = 6.8 6.8 - 1
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 200933 None 0 Human Binding pKi = 6.8 6.8 - 1
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 200933 None 0 Human Binding pKi = 6.8 6.8 - 1
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 94950 None 1 Human Binding pKi = 5.8 5.8 - 1
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 94950 None 1 Human Binding pKi = 5.8 5.8 - 1
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 210980 None 0 Rat Binding pKi = 7.8 7.8 - 1
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 199478 None 0 Human Binding pKi = 7.8 7.8 - 1
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 199478 None 0 Human Binding pKi = 7.8 7.8 - 1
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 199647 None 0 Human Binding pKi = 7.8 7.8 - 1
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 199647 None 0 Human Binding pKi = 7.8 7.8 - 1
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 190658 None 0 Human Binding pKi = 7.8 7.8 - 1
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 190658 None 0 Human Binding pKi = 7.8 7.8 - 1
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 214703 None 0 Human Binding pKi = 7.7 7.7 - 1
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 216628 None 0 Human Binding pKi = 7.7 7.7 - 1
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 193246 None 0 Human Binding pKi = 7.7 7.7 - 1
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 193246 None 0 Human Binding pKi = 7.7 7.7 - 1
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 68052 None 0 Human Binding pKi = 6.7 6.7 - 1
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 68052 None 0 Human Binding pKi = 6.7 6.7 - 1
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 188044 None 0 Cat Binding pKi = 6.7 6.7 -31 2
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 188044 None 0 Cat Binding pKi = 6.7 6.7 -31 2
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 95294 None 0 Human Binding pKi = 6.7 6.7 - 1
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 95294 None 0 Human Binding pKi = 6.7 6.7 - 1
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 95372 None 0 Human Binding pKi = 6.7 6.7 - 1
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 95372 None 0 Human Binding pKi = 6.7 6.7 - 1
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 155533 None 0 Human Binding pKi = 6.7 6.7 - 1
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 155533 None 0 Human Binding pKi = 6.7 6.7 - 1
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 67611 None 0 Human Binding pKi = 5.7 5.7 - 1
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 67611 None 0 Human Binding pKi = 5.7 5.7 - 1
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 171115 None 0 Human Binding pKi = 5.7 5.7 - 1
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 171115 None 0 Human Binding pKi = 5.7 5.7 - 1
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 95714 None 0 Human Binding pKi = 5.7 5.7 - 1
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 95714 None 0 Human Binding pKi = 5.7 5.7 - 1
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 214675 None 2 Human Binding pKi = 5.7 5.7 - 1
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 95653 None 0 Human Binding pKi = 8.7 8.7 - 1
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 95653 None 0 Human Binding pKi = 8.7 8.7 - 1
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 155295 None 0 Human Binding pKi = 8.7 8.7 - 1
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 155295 None 0 Human Binding pKi = 8.7 8.7 - 1
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 173419 None 0 Human Binding pKi = 8.7 8.7 - 1
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 173419 None 0 Human Binding pKi = 8.7 8.7 - 1
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 211860 None 0 Human Binding pKi = 8.7 8.7 - 1
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 213832 None 0 Human Binding pKi = 8.7 8.7 - 1
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 213098 None 0 Human Binding pKi = 8.6 8.6 - 1
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 218112 None 0 Human Binding pKi = 8.6 8.6 - 1
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 211799 None 0 Human Binding pKi = 8.5 8.5 - 1
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 176141 None 0 Human Binding pKi = 8.5 8.5 - 1
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 176141 None 0 Human Binding pKi = 8.5 8.5 - 1
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 213149 None 0 Human Binding pKi = 8.5 8.5 - 1
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 186826 None 0 Human Binding pKi = 7.7 7.7 - 1
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 186826 None 0 Human Binding pKi = 7.7 7.7 - 1
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 172449 None 0 Human Binding pKi = 7.7 7.7 - 1
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 172449 None 0 Human Binding pKi = 7.7 7.7 - 1
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 210982 None 0 Rat Binding pKi = 6.7 6.7 - 1
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 199889 None 0 Human Binding pKi = 6.7 6.7 - 1
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 199889 None 0 Human Binding pKi = 6.7 6.7 - 1
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 3526 None 17 Human Binding pKi = 6.7 6.7 -1 3
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 174388 None 0 Human Binding pKi = 5.7 5.7 - 1
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 174388 None 0 Human Binding pKi = 5.7 5.7 - 1
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 171021 None 0 Human Binding pKi = 5.7 5.7 - 1
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 171021 None 0 Human Binding pKi = 5.7 5.7 - 1
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 216679 None 0 Human Binding pKi = 6.7 6.7 - 1
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 172359 None 0 Human Binding pKi = 7.6 7.6 - 1
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 172359 None 0 Human Binding pKi = 7.6 7.6 - 1
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 175185 None 0 Human Binding pKi = 6.6 6.6 - 1
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 175185 None 0 Human Binding pKi = 6.6 6.6 - 1
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 211871 None 0 Human Binding pKi = 7.6 7.6 - 1
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 200213 None 0 Human Binding pKi = 6.6 6.6 - 1
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 200213 None 0 Human Binding pKi = 6.6 6.6 - 1
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 183638 None 0 Human Binding pKi = 6.6 6.6 - 1
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 183638 None 0 Human Binding pKi = 6.6 6.6 - 1
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 170478 None 0 Human Binding pKi = 6.6 6.6 - 1
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 170478 None 0 Human Binding pKi = 6.6 6.6 - 1
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 201019 None 0 Human Binding pKi = 7.6 7.6 - 1
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 201019 None 0 Human Binding pKi = 7.6 7.6 - 1
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 95557 None 0 Human Binding pKi = 7.6 7.6 - 1
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 95557 None 0 Human Binding pKi = 7.6 7.6 - 1
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 187990 None 0 Human Binding pKi = 7.6 7.6 15 2
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 187990 None 0 Human Binding pKi = 7.6 7.6 15 2
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 189187 None 0 Human Binding pKi = 7.6 7.6 - 1
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 189187 None 0 Human Binding pKi = 7.6 7.6 - 1
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 186824 None 0 Human Binding pKi = 5.6 5.6 - 1
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 186824 None 0 Human Binding pKi = 5.6 5.6 - 1
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 3526 None 17 Rhesus macaque Binding pKi = 6.6 6.6 -1 3
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 3526 None 17 Rhesus macaque Binding pKi = 6.6 6.6 -1 3
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 3526 None 17 Rhesus macaque Binding pKi = 6.6 6.6 -1 3
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 135255 None 0 Human Binding pKi = 6.6 6.6 - 1
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 135255 None 0 Human Binding pKi = 6.6 6.6 - 1
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 95601 None 0 Human Binding pKi = 6.6 6.6 - 1
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 95601 None 0 Human Binding pKi = 6.6 6.6 - 1
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 67526 None 0 Human Binding pKi = 5.6 5.6 - 1
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 67526 None 0 Human Binding pKi = 5.6 5.6 - 1
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 135655 None 0 Human Binding pKi = 5.6 5.6 - 1
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 135655 None 0 Human Binding pKi = 5.6 5.6 - 1
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 160142 None 0 Human Binding pKi = 5.6 5.6 - 1
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 160142 None 0 Human Binding pKi = 5.6 5.6 - 1
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 161954 None 0 Human Binding pKi = 5.6 5.6 - 1
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 161954 None 0 Human Binding pKi = 5.6 5.6 - 1
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 188124 None 0 Cat Binding pKi = 5.6 5.6 -89 2
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 188124 None 0 Cat Binding pKi = 5.6 5.6 -89 2
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 155297 None 0 Human Binding pKi = 5.6 5.6 - 1
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 155297 None 0 Human Binding pKi = 5.6 5.6 - 1
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 188883 None 0 Human Binding pKi = 5.6 5.6 - 1
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 188883 None 0 Human Binding pKi = 5.6 5.6 - 1
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 216680 None 0 Human Binding pKi = 7.6 7.6 - 1
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 3961 None 0 Human Binding pKi = 6.6 6.6 - 1
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 3961 None 0 Human Binding pKi = 6.6 6.6 - 1
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 3961 None 0 Human Binding pKi = 6.6 6.6 - 1
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 89928 None 0 Human Binding pKi = 7.6 7.6 - 1
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 89928 None 0 Human Binding pKi = 7.6 7.6 - 1
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 199426 None 0 Human Binding pKi = 6.6 6.6 - 1
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 199426 None 0 Human Binding pKi = 6.6 6.6 - 1
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 199832 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199832 None 0 Human Binding pKi = 6.5 6.5 - 1
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 172718 None 0 Human Binding pKi = 8.5 8.5 - 1
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 172718 None 0 Human Binding pKi = 8.5 8.5 - 1
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 173614 None 0 Human Binding pKi = 8.5 8.5 - 1
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 173614 None 0 Human Binding pKi = 8.5 8.5 - 1
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 95468 None 0 Human Binding pKi = 8.5 8.5 - 1
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 95468 None 0 Human Binding pKi = 8.5 8.5 - 1
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 183160 None 0 Human Binding pKi = 8.5 8.5 - 1
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 183160 None 0 Human Binding pKi = 8.5 8.5 - 1
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 3526 None 17 Rat Binding pKi = 8.5 8.5 1 3
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 3526 None 17 Rat Binding pKi = 8.5 8.5 1 3
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 3526 None 17 Rat Binding pKi = 8.5 8.5 1 3
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 170996 None 0 Human Binding pKi = 8.5 8.5 - 1
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 170996 None 0 Human Binding pKi = 8.5 8.5 - 1
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 171535 None 0 Human Binding pKi = 8.5 8.5 - 1
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 171535 None 0 Human Binding pKi = 8.5 8.5 - 1
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 216798 None 0 Human Binding pKi = 8.4 8.4 - 1
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 155598 None 0 Human Binding pKi = 8.4 8.4 1 2
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 155598 None 0 Human Binding pKi = 8.4 8.4 1 2
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 188077 None 0 Human Binding pKi = 8.4 8.4 31 2
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 188077 None 0 Human Binding pKi = 8.4 8.4 31 2
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 188078 None 0 Human Binding pKi = 8.4 8.4 100 2
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 188078 None 0 Human Binding pKi = 8.4 8.4 100 2
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 90854 None 0 Human Binding pKi = 7.5 7.5 - 1
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 90854 None 0 Human Binding pKi = 7.5 7.5 - 1
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 90918 None 0 Human Binding pKi = 7.5 7.5 - 1
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 90918 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95198 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95198 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95293 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95293 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95300 None 0 Human Binding pKi = 7.5 7.5 - 1
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 95300 None 0 Human Binding pKi = 7.5 7.5 - 1
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 188137 None 0 Human Binding pKi = 7.5 7.5 - 1
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 188137 None 0 Human Binding pKi = 7.5 7.5 - 1
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 199313 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199313 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199393 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199393 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199400 None 0 Human Binding pKi = 6.5 6.5 - 1
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 199400 None 0 Human Binding pKi = 6.5 6.5 - 1
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 96828 None 0 Human Binding pKi = 6.5 6.5 - 1
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 96828 None 0 Human Binding pKi = 6.5 6.5 - 1
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 187913 None 0 Human Binding pKi = 6.5 6.5 - 1
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 187913 None 0 Human Binding pKi = 6.5 6.5 - 1
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 3526 None 17 Rat Binding pKi = 5.5 5.5 1 3
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 3526 None 17 Rat Binding pKi = 5.5 5.5 1 3
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 3526 None 17 Rat Binding pKi = 5.5 5.5 1 3
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 67848 None 0 Human Binding pKi = 5.5 5.5 - 1
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 67848 None 0 Human Binding pKi = 5.5 5.5 - 1
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 161548 None 0 Human Binding pKi = 5.5 5.5 - 1
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 161548 None 0 Human Binding pKi = 5.5 5.5 - 1
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 169106 None 0 Human Binding pKi = 5.5 5.5 - 1
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 169106 None 0 Human Binding pKi = 5.5 5.5 - 1
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 199294 None 0 Human Binding pKi = 7.5 7.5 - 1
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 199294 None 0 Human Binding pKi = 7.5 7.5 - 1
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 96828 None 0 Human Binding pKi = 6.5 6.5 - 1
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 96828 None 0 Human Binding pKi = 6.5 6.5 - 1
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 201375 None 0 Human Binding pKi = 5.5 5.5 - 1
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 201375 None 0 Human Binding pKi = 5.5 5.5 - 1
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 199407 None 0 Human Binding pKi = 7.5 7.5 - 1
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 199407 None 0 Human Binding pKi = 7.5 7.5 - 1
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 183707 None 0 Human Binding pKi = 6.5 6.5 - 1
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 183707 None 0 Human Binding pKi = 6.5 6.5 - 1
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 184158 None 0 Human Binding pKi = 5.5 5.5 - 1
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 184158 None 0 Human Binding pKi = 5.5 5.5 - 1
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 191774 None 0 Human Binding pKi = 7.4 7.4 - 1
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 191774 None 0 Human Binding pKi = 7.4 7.4 - 1
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 184113 None 0 Human Binding pKi = 6.4 6.4 - 1
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 184113 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69413 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69413 None 0 Human Binding pKi = 6.4 6.4 - 1
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 127468 None 0 Human Binding pKi = 6.4 6.4 - 1
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 127468 None 0 Human Binding pKi = 6.4 6.4 - 1
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 133684 None 0 Human Binding pKi = 6.4 6.4 - 1
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 133684 None 0 Human Binding pKi = 6.4 6.4 - 1
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 188078 None 0 Cat Binding pKi = 6.4 6.4 -100 2
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 188078 None 0 Cat Binding pKi = 6.4 6.4 -100 2
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 94904 None 0 Human Binding pKi = 6.4 6.4 - 1
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 94904 None 0 Human Binding pKi = 6.4 6.4 - 1
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 94951 None 1 Human Binding pKi = 6.4 6.4 - 1
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 94951 None 1 Human Binding pKi = 6.4 6.4 - 1
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 216308 None 0 Human Binding pKi = 6.4 6.4 - 1
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 94875 None 0 Human Binding pKi = 5.4 5.4 - 1
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 94875 None 0 Human Binding pKi = 5.4 5.4 - 1
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 187912 None 0 Human Binding pKi = 5.4 5.4 - 1
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 187912 None 0 Human Binding pKi = 5.4 5.4 - 1
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 189015 None 7 Human Binding pKi = 8.4 8.4 - 1
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 189015 None 7 Human Binding pKi = 8.4 8.4 - 1
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 2995 None 41 Rhesus macaque Binding pKi = 8.4 8.4 3 6
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 2995 None 41 Rhesus macaque Binding pKi = 8.4 8.4 3 6
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 2995 None 41 Rhesus macaque Binding pKi = 8.4 8.4 3 6
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 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 199743 None 0 Human Binding pKi = 8.4 8.4 - 1
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 199743 None 0 Human Binding pKi = 8.4 8.4 - 1
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 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 210992 None 0 Rat Binding pKi = 8.4 8.4 - 1
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 211862 None 0 Human Binding pKi = 8.3 8.3 - 1
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 155639 None 0 Human Binding pKi = 7.4 7.4 - 1
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 155639 None 0 Human Binding pKi = 7.4 7.4 - 1
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 1979 None 5 Human Binding pKi = 5.4 5.4 -91201 4
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 1979 None 5 Human Binding pKi = 5.4 5.4 -91201 4
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 1979 None 5 Human Binding pKi = 5.4 5.4 -91201 4
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 211857 None 0 Human Binding pKi = 6.4 6.4 1 2
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 2995 None 41 Human Binding pKi = 7.4 7.4 -3 6
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 2995 None 41 Human Binding pKi = 7.4 7.4 -3 6
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 2995 None 41 Human Binding pKi = 7.4 7.4 -3 6
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 190868 None 0 Human Binding pKi = 7.4 7.4 - 1
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 190868 None 0 Human Binding pKi = 7.4 7.4 - 1
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 183706 None 0 Human Binding pKi = 7.4 7.4 - 1
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 183706 None 0 Human Binding pKi = 7.4 7.4 - 1
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 146481 None 0 Human Binding pKi = 6.4 6.4 - 1
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 146481 None 0 Human Binding pKi = 6.4 6.4 - 1
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 199601 None 0 Human Binding pKi = 6.4 6.4 - 1
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 199601 None 0 Human Binding pKi = 6.4 6.4 - 1
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 200194 None 0 Human Binding pKi = 7.4 7.4 - 1
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 200194 None 0 Human Binding pKi = 7.4 7.4 - 1
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 189947 None 0 Human Binding pKi = 7.4 7.4 - 1
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 189947 None 0 Human Binding pKi = 7.4 7.4 - 1
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 199578 None 0 Human Binding pKi = 7.4 7.4 - 1
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 199578 None 0 Human Binding pKi = 7.4 7.4 - 1
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 197217 None 0 Human Binding pKi = 7.3 7.3 - 1
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 197217 None 0 Human Binding pKi = 7.3 7.3 - 1
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 170639 None 0 Human Binding pKi = 7.3 7.3 - 1
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 170639 None 0 Human Binding pKi = 7.3 7.3 - 1
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 199229 None 0 Human Binding pKi = 7.3 7.3 - 1
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 199229 None 0 Human Binding pKi = 7.3 7.3 - 1
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 199660 None 0 Human Binding pKi = 7.3 7.3 - 1
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 199660 None 0 Human Binding pKi = 7.3 7.3 - 1
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 2995 None 41 Human Binding pKi = 8.3 8.3 -3 6
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 2995 None 41 Human Binding pKi = 8.3 8.3 -3 6
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 2995 None 41 Human Binding pKi = 8.3 8.3 -3 6
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 173697 None 0 Human Binding pKi = 8.3 8.3 - 1
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 173697 None 0 Human Binding pKi = 8.3 8.3 - 1
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 95412 None 0 Human Binding pKi = 8.3 8.3 - 1
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 95412 None 0 Human Binding pKi = 8.3 8.3 - 1
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 95512 None 0 Human Binding pKi = 8.3 8.3 - 1
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 95512 None 0 Human Binding pKi = 8.3 8.3 - 1
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 211905 None 12 Human Binding pKi = 8.3 8.3 1 2
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 211905 None 12 Human Binding pKi = 8.3 8.3 1 2
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 211905 None 12 Human Binding pKi = 8.3 8.3 1 2
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 3535 None 23 Human Binding pKi = 8.3 8.3 2 3
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 3535 None 23 Human Binding pKi = 8.3 8.3 2 3
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 3535 None 23 Human Binding pKi = 8.3 8.3 2 3
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 184160 None 0 Human Binding pKi = 8.3 8.3 - 1
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 184160 None 0 Human Binding pKi = 8.3 8.3 - 1
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 95337 None 0 Human Binding pKi = 7.3 7.3 - 1
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 95337 None 0 Human Binding pKi = 7.3 7.3 - 1
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 187911 None 0 Human Binding pKi = 7.3 7.3 12 2
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 187911 None 0 Human Binding pKi = 7.3 7.3 12 2
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 188135 None 0 Human Binding pKi = 7.3 7.3 - 1
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 188135 None 0 Human Binding pKi = 7.3 7.3 - 1
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 183999 None 0 Human Binding pKi = 6.3 6.3 - 1
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 183999 None 0 Human Binding pKi = 6.3 6.3 - 1
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 67972 None 0 Human Binding pKi = 6.3 6.3 - 1
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 67972 None 0 Human Binding pKi = 6.3 6.3 - 1
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 69198 None 0 Human Binding pKi = 6.3 6.3 - 1
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 69198 None 0 Human Binding pKi = 6.3 6.3 - 1
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 126449 None 1 Human Binding pKi = 6.3 6.3 - 1
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 126449 None 1 Human Binding pKi = 6.3 6.3 - 1
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 95081 None 0 Human Binding pKi = 6.3 6.3 - 1
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 95081 None 0 Human Binding pKi = 6.3 6.3 - 1
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 95425 None 0 Human Binding pKi = 6.3 6.3 - 1
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 95425 None 0 Human Binding pKi = 6.3 6.3 - 1
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 175035 None 0 Human Binding pKi = 5.3 5.3 - 1
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 175035 None 0 Human Binding pKi = 5.3 5.3 - 1
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 145438 None 0 Human Binding pKi = 7.3 7.3 - 1
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 145438 None 0 Human Binding pKi = 7.3 7.3 - 1
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 199637 None 0 Human Binding pKi = 6.3 6.3 - 1
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 199637 None 0 Human Binding pKi = 6.3 6.3 - 1
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 200268 None 0 Human Binding pKi = 6.2 6.2 - 1
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 200268 None 0 Human Binding pKi = 6.2 6.2 - 1
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 199620 None 0 Human Binding pKi = 7.2 7.2 - 1
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 199620 None 0 Human Binding pKi = 7.2 7.2 - 1
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 201016 None 0 Human Binding pKi = 7.2 7.2 - 1
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 201016 None 0 Human Binding pKi = 7.2 7.2 - 1
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 155262 None 1 Human Binding pKi = 8.2 8.2 -1 2
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 155262 None 1 Human Binding pKi = 8.2 8.2 -1 2
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 188352 None 0 Human Binding pKi = 8.2 8.2 - 1
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 188352 None 0 Human Binding pKi = 8.2 8.2 - 1
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 95155 None 0 Human Binding pKi = 8.2 8.2 - 1
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 95155 None 0 Human Binding pKi = 8.2 8.2 - 1
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 95761 None 0 Human Binding pKi = 8.2 8.2 - 1
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 95761 None 0 Human Binding pKi = 8.2 8.2 - 1
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 213522 None 7 Human Binding pKi = 8.2 8.2 - 1
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 155262 None 1 Human Binding pKi = 8.2 8.2 -1 2
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 155262 None 1 Human Binding pKi = 8.2 8.2 -1 2
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 188044 None 0 Human Binding pKi = 8.2 8.2 31 2
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 188044 None 0 Human Binding pKi = 8.2 8.2 31 2
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 188124 None 0 Human Binding pKi = 8.2 8.2 89 2
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 188124 None 0 Human Binding pKi = 8.2 8.2 89 2
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 155262 None 1 Rat Binding pKi = 8.2 8.2 1 2
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 155262 None 1 Rat Binding pKi = 8.2 8.2 1 2
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 216446 None 0 Human Binding pKi = 8.2 8.2 - 1
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 213826 None 0 Human Binding pKi = 8.2 8.2 - 1
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 183954 None 0 Human Binding pKi = 7.2 7.2 - 1
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 183954 None 0 Human Binding pKi = 7.2 7.2 - 1
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 210983 None 0 Rat Binding pKi = 6.2 6.2 - 1
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 199340 None 0 Human Binding pKi = 7.2 7.2 - 1
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 199340 None 0 Human Binding pKi = 7.2 7.2 - 1
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 184109 None 0 Human Binding pKi = 7.2 7.2 - 1
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 184109 None 0 Human Binding pKi = 7.2 7.2 - 1
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 95558 None 0 Human Binding pKi = 7.2 7.2 - 1
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 95558 None 0 Human Binding pKi = 7.2 7.2 - 1
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 188134 None 0 Human Binding pKi = 7.2 7.2 - 1
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 188134 None 0 Human Binding pKi = 7.2 7.2 - 1
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 188865 None 0 Human Binding pKi = 7.2 7.2 - 1
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 188865 None 0 Human Binding pKi = 7.2 7.2 - 1
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 173319 None 0 Human Binding pKi = 6.2 6.2 - 1
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 173319 None 0 Human Binding pKi = 6.2 6.2 - 1
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 173497 None 0 Human Binding pKi = 6.2 6.2 - 1
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 173497 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69403 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69403 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69422 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69422 None 0 Human Binding pKi = 6.2 6.2 - 1
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 122421 None 0 Human Binding pKi = 6.2 6.2 - 1
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 122421 None 0 Human Binding pKi = 6.2 6.2 - 1
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 135350 None 0 Human Binding pKi = 6.2 6.2 - 1
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 135350 None 0 Human Binding pKi = 6.2 6.2 - 1
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 187911 None 0 Cat Binding pKi = 6.2 6.2 -12 2
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 187911 None 0 Cat Binding pKi = 6.2 6.2 -12 2
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 188077 None 0 Cat Binding pKi = 6.2 6.2 -31 2
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 188077 None 0 Cat Binding pKi = 6.2 6.2 -31 2
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 95197 None 0 Human Binding pKi = 6.2 6.2 - 1
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 95197 None 0 Human Binding pKi = 6.2 6.2 - 1
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 199457 None 0 Human Binding pKi = 7.2 7.2 -25 2
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 199457 None 0 Human Binding pKi = 7.2 7.2 -25 2
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 199457 None 0 Human Binding pKi = 7.2 7.2 -25 2
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 199457 None 0 Human Binding pKi = 7.2 7.2 -25 2
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 151811 None 0 Human Binding pKi = 7.2 7.2 - 1
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 151811 None 0 Human Binding pKi = 7.2 7.2 - 1
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 184131 None 0 Human Binding pKi = 7.2 7.2 - 1
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 184131 None 0 Human Binding pKi = 7.2 7.2 - 1
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 218303 None 7 Human Binding pKi = 8.1 8.1 - 1
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 155559 None 0 Human Binding pKi = 8.1 8.1 - 1
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 155559 None 0 Human Binding pKi = 8.1 8.1 - 1
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 155598 None 0 Human Binding pKi = 8.1 8.1 1 2
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 155598 None 0 Human Binding pKi = 8.1 8.1 1 2
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 199348 None 0 Human Binding pKi = 6.2 6.2 - 1
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 199348 None 0 Human Binding pKi = 6.2 6.2 - 1
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 192657 None 0 Human Binding pKi = 7.2 7.2 - 1
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 192657 None 0 Human Binding pKi = 7.2 7.2 - 1
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 215950 None 0 Human Binding pKi = 7.1 7.1 - 1
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 199690 None 0 Human Binding pKi = 7.1 7.1 - 1
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 199690 None 0 Human Binding pKi = 7.1 7.1 - 1
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 91783 None 0 Human Binding pKi = 7.1 7.1 - 1
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 91783 None 0 Human Binding pKi = 7.1 7.1 - 1
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 155347 None 0 Human Binding pKi = 7.1 7.1 - 1
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 155347 None 0 Human Binding pKi = 7.1 7.1 - 1
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 95325 None 0 Human Binding pKi = 7.1 7.1 - 1
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 95325 None 0 Human Binding pKi = 7.1 7.1 - 1
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 95326 None 0 Human Binding pKi = 7.1 7.1 - 1
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 95326 None 0 Human Binding pKi = 7.1 7.1 - 1
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 155263 None 0 Human Binding pKi = 7.1 7.1 - 1
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 155263 None 0 Human Binding pKi = 7.1 7.1 - 1
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 187736 None 0 Human Binding pKi = 7.1 7.1 - 1
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 187736 None 0 Human Binding pKi = 7.1 7.1 - 1
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 193512 None 0 Human Binding pKi = 7.1 7.1 - 1
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 193512 None 0 Human Binding pKi = 7.1 7.1 - 1
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 67534 None 0 Human Binding pKi = 6.1 6.1 - 1
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 67534 None 0 Human Binding pKi = 6.1 6.1 - 1
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 94903 None 0 Human Binding pKi = 6.1 6.1 - 1
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 94903 None 0 Human Binding pKi = 6.1 6.1 - 1
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 95597 None 0 Human Binding pKi = 6.1 6.1 - 1
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 95597 None 0 Human Binding pKi = 6.1 6.1 - 1
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 155621 None 0 Human Binding pKi = 6.1 6.1 - 1
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 155621 None 0 Human Binding pKi = 6.1 6.1 - 1
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 188108 None 0 Human Binding pKi = 6.1 6.1 - 1
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 188108 None 0 Human Binding pKi = 6.1 6.1 - 1
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 192854 None 0 Human Binding pKi = 6.1 6.1 - 1
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 192854 None 0 Human Binding pKi = 6.1 6.1 - 1
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 193169 None 0 Human Binding pKi = 6.1 6.1 - 1
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 193169 None 0 Human Binding pKi = 6.1 6.1 - 1
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 95082 None 0 Human Binding pKi = 5.1 5.1 - 1
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 95082 None 0 Human Binding pKi = 5.1 5.1 - 1
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 95522 None 0 Human Binding pKi = 5.1 5.1 - 1
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 95522 None 0 Human Binding pKi = 5.1 5.1 - 1
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 95460 None 0 Human Binding pKi = 8.1 8.1 - 1
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 95460 None 0 Human Binding pKi = 8.1 8.1 - 1
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 3535 None 23 Human Binding pKi = 8.1 8.1 2 3
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 3535 None 23 Human Binding pKi = 8.1 8.1 2 3
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 3535 None 23 Human Binding pKi = 8.1 8.1 2 3
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 200206 None 0 Human Binding pKi = 8.1 8.1 - 1
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 200206 None 0 Human Binding pKi = 8.1 8.1 - 1
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 171843 None 0 Human Binding pKi = 6.1 6.1 - 1
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 171843 None 0 Human Binding pKi = 6.1 6.1 - 1
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 199225 None 0 Human Binding pKi = 7.1 7.1 - 1
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 199225 None 0 Human Binding pKi = 7.1 7.1 - 1
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 214775 None 0 Human Binding pKi = 8.0 8.0 - 1
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 216633 None 0 Human Binding pKi = 8.0 8.0 - 1
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 217732 None 0 Human Binding pKi = 8.0 8.0 - 1
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 216670 None 0 Human Binding pKi = 8.0 8.0 - 1
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 199940 None 0 Human Binding pKi = 7.0 7.0 - 1
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 199940 None 0 Human Binding pKi = 7.0 7.0 - 1
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 191315 None 0 Human Binding pKi = 7.0 7.0 - 1
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 191315 None 0 Human Binding pKi = 7.0 7.0 - 1
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 3295 None 0 Human Binding pIC50 = 9 9.0 - 0
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 3295 None 0 Human Binding pIC50 = 9 9.0 - 0
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 None 0 Human Binding pKd = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
11995575 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
11995575 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2156 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
2156 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
CHEMBL437110 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
CHEMBL437110 3961 None 0 Human Binding pKd = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2162 649 None 0 Human Binding pKd None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12770925
2166 3844 None 0 Human Binding pKd None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
24893978 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 1010 None 6 Human Binding pKi = 8.4 8.4 9 8
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 907 None 0 Rat Binding pKi = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17125276
2151 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
2151 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
9797568 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
9797568 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
CHEMBL192359 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
CHEMBL192359 244 None 10 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
10278166 3528 None 33 Human Binding pKi = 6.6 6.6 -2 2
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 3528 None 33 Human Binding pKi = 6.6 6.6 -2 2
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 3528 None 33 Human Binding pKi = 6.6 6.6 -2 2
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 3526 None 17 Rat Binding pKi = 6.7 6.7 1 3
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 3526 None 17 Rat Binding pKi = 6.7 6.7 1 3
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 3526 None 17 Rat Binding pKi = 6.7 6.7 1 3
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 2967 None 0 Rat Binding pKi = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
9438 2967 None 0 Rat Binding pKi = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
21023902 3535 None 23 Human Binding pKi = 8 8.0 2 3
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 3535 None 23 Human Binding pKi = 8 8.0 2 3
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 3535 None 23 Human Binding pKi = 8 8.0 2 3
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 3948 None 0 Human Binding pKi = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14645137
25126427 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 2141 None 6 Human Binding pKi = 8.4 8.4 - 1
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 3960 None 0 Human Binding pKi = 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10499587
2153 3960 None 0 Human Binding pKi = 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10548501
2153 3960 None 0 Human Binding pKi = 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10559967
2153 3960 None 0 Human Binding pKi = 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10581185
10213684 3935 None 0 Human Binding pKi = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2152 3935 None 0 Human Binding pKi = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
CHEMBL414256 3935 None 0 Human Binding pKi = 9.6 9.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2160 3042 None 0 Human Binding pKi = 9.7 9.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
21023902 3535 None 23 Mouse Binding pKi None 7.7 7.7 -2 3
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 3535 None 23 Rat Binding pKi None 7.7 7.7 -2 3
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 3535 None 23 Mouse Binding pKi None 7.7 7.7 -2 3
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 3535 None 23 Rat Binding pKi None 7.7 7.7 -2 3
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 3535 None 23 Mouse Binding pKi None 7.7 7.7 -2 3
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 3535 None 23 Rat Binding pKi None 7.7 7.7 -2 3
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 3958 None 0 Mouse Binding pKi None 8.5 8.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2154 3958 None 0 Mouse Binding pKi None 8.5 8.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3958 None 0 Human Binding pKi None 8.5 8.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 None 0 Human Binding pKi None 8.5 8.5 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3960 None 0 Mouse Binding pKi None 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2153 3960 None 0 Mouse Binding pKi None 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 None 0 Mouse Binding pKi None 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2155 3959 None 0 Mouse Binding pKi None 8.6 8.6 -1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3960 None 0 Rat Binding pKi None 8.7 8.7 1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3958 None 0 Rat Binding pKi None 8.8 8.8 1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 None 0 Rat Binding pKi None 8.8 8.8 1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2159 761 None 0 Human Binding pKi None 9.1 9.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12495432