Ligand source activities (1 row/activity)



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

 p-value
(-log)		 Activity
Type		 Activity
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CHEMBL218994 209403 0 None 1 2 Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165734 208527 0 None - 1 Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163460 208518 0 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163463 208519 7 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 212437 1 None - 1 Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163467 208520 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165797 208534 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165767 208530 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44189349 181795 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181795 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL577772 215777 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 215777 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1165735 208528 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL504097 214174 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163473 208522 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
162650062 180090 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4748168 180090 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL437430 213718 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1016/j.bmc.2009.07.058
145965592 164416 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 164416 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973990 164685 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL524855 215622 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL510618 215585 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162646037 179514 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 179514 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL1165796 208533 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL1165793 208531 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm901294u
CHEMBL1165794 208532 1 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL2372899 210304 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL385616 212358 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(=O)O 10.1021/jm0111043
CHEMBL53181 215708 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372897 210303 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
145967082 164101 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162663320 182017 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780734 182017 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
162648628 179855 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179855 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593663 215814 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
162644923 179429 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 179429 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
145978068 163736 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163736 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164729 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164729 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL406590 212615 0 None - 1 Human 6.0 pEC50 = 6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL505358 214192 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162655718 180697 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4755542 180697 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24953411 14083 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197619 14083 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL578654 14083 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
162668637 182647 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182647 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
24952710 14068 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197510 14068 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574732 14068 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953059 14065 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197507 14065 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574726 14065 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
162660425 181298 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762329 181298 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163990 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
2151 244 9 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
9797568 244 9 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
CHEMBL192359 244 9 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
15983447 85647 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228413 85647 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
15983564 85666 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228525 85666 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
10407901 10844 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172234 10844 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799325 14383 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173106 14383 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200251 14383 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
145967082 164101 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163990 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
46897997 14366 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172407 14366 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200175 14366 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
145965592 164416 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 164416 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607810 215833 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163686 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24954831 14063 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197503 14063 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574527 14063 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163990 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163990 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145965592 164416 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 164416 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953055 14052 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197455 14052 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572883 14052 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
11983241 85655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228470 85655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL607811 215834 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163686 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372905 210310 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
11325792 140167 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
CHEMBL380346 140167 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
15983822 85846 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229713 85846 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162666444 182272 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783832 182272 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
49799029 14386 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173147 14386 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200258 14386 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983820 161747 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL413787 161747 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
162664787 182214 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783104 182214 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 211063 7 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44409467 74755 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL203080 74755 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572699 74755 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799289 14396 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1173399 14396 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200283 14396 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
145966260 164386 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 164386 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372904 210309 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977223 163990 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162671682 182889 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182889 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
15983443 137334 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL375275 137334 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
15983686 138086 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376582 138086 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
162649626 180067 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4747883 180067 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163990 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608099 215837 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
15983445 85646 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228412 85646 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145973990 164685 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49798987 14370 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172604 14370 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200193 14370 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
15983693 169393 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL442230 169393 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162669582 182729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789784 182729 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
145973104 164729 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164729 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11524599 76727 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL206596 76727 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145978068 163736 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163736 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372903 210308 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799280 14390 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173239 14390 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200268 14390 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
24954830 14046 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197440 14046 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572398 14046 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
15983690 85916 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229924 85916 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163471 208521 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL298803 210904 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm0111043
CHEMBL427632 213358 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL408106 212701 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL426020 213343 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2372896 210302 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145967082 164101 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608098 215836 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
162662463 182033 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780893 182033 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
24795079 14053 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197471 14053 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573392 14053 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
46897998 14355 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1172180 14355 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1200148 14355 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
46897996 14364 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1172224 14364 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1200156 14364 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
15983570 85872 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229868 85872 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
162670598 182922 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182922 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL2372895 210301 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799327 14387 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173170 14387 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200259 14387 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162677235 183495 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 183495 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 244 9 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
9797568 244 9 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL192359 244 9 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL1163477 208524 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46897995 14363 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1172223 14363 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200155 14363 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
145966260 164386 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 164386 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24955192 14062 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197496 14062 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574305 14062 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
145977223 163990 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799291 14397 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173400 14397 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200284 14397 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162653594 180538 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4753729 180538 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
49799368 14375 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172764 14375 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200219 14375 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983449 85654 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228461 85654 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
10213684 3935 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
2152 3935 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL414256 3935 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372907 210311 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163686 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372902 210307 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)CCC(=O)O)C(=O)O 10.1021/jm0111043
CHEMBL1627325 208811 0 None -102 8 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
162657061 180900 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180900 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL216349 209326 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1)C(=O)O 10.1021/jm0111043
CHEMBL3104471 211063 7 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
10996495 179912 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL4746051 179912 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL385962 212370 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162649156 179828 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745061 179828 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 244 9 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
9797568 244 9 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
CHEMBL192359 244 9 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
24952707 14044 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197438 14044 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572391 14044 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983691 85820 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229659 85820 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163475 208523 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
145973104 164729 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164729 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
45481596 14077 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197565 14077 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL576746 14077 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
11696838 77156 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL207823 77156 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573857 77156 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 164386 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 164386 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 181293 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 181293 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162644289 181791 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777923 181791 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
145973990 164685 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953056 14072 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197533 14072 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575629 14072 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
145965592 164416 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 164416 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953060 14047 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197441 14047 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572423 14047 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163990 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977587 163686 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145967082 164101 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145978068 163736 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163736 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24952352 14058 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197480 14058 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573575 14058 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1163479 208525 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
15983818 85845 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229710 85845 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164685 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983826 85847 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229714 85847 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
24953414 14060 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197484 14060 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573836 14060 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799486 14403 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173689 14403 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200298 14403 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983560 85656 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228471 85656 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL593662 215813 9 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900604g
162651887 180271 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 180271 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162645261 179685 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4743591 179685 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
10474282 69112 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL192389 69112 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
49798794 14334 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1170888 14334 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200021 14334 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983562 85657 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228472 85657 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
16126405 137178 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL374817 137178 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
24953410 14048 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197442 14048 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572439 14048 5 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
24952350 14093 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197698 14093 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL582835 14093 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983688 85915 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229923 85915 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
45481598 14059 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197481 14059 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573640 14059 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
16126557 85855 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229764 85855 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983568 138084 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376581 138084 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
145965592 164416 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 164416 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164729 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164729 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL437430 213718 0 None 3 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL452403 213981 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
145973990 164685 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372901 210306 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162666856 182474 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4786585 182474 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
10340786 71316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL195746 71316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
46897993 14389 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1173172 14389 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1200261 14389 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
44409548 77329 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL208362 77329 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL573837 77329 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
46897999 14354 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1171808 14354 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200120 14354 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
15983558 142033 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL387661 142033 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
24953412 14084 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197628 14084 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL578853 14084 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
49799329 14388 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173171 14388 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200260 14388 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL412753 213023 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163686 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953058 14074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197539 14074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL575819 14074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
15983684 85914 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229922 85914 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
24952349 14056 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197478 14056 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573570 14056 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
24952351 14066 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197508 14066 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574730 14066 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
15983695 144617 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL390792 144617 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983824 142036 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL387694 142036 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983566 85667 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228526 85667 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL501794 214145 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1165764 208529 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
145967082 164101 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL3104471 211063 7 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607809 215832 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
162666100 182269 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783820 182269 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163990 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983816 85844 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229709 85844 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164685 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164685 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44400855 135285 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL372689 135285 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
45482441 14057 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197479 14057 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573574 14057 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
24952709 14067 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197509 14067 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574731 14067 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953413 14078 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197568 14078 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL576922 14078 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
162658232 180988 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4758767 180988 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
45481583 14050 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197444 14050 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572467 14050 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
145967082 164101 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 164101 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799366 14374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172763 14374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200218 14374 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
46897994 14399 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1173492 14399 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200286 14399 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
145978068 163736 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163736 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163990 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL508811 215140 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
49799023 14382 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173081 14382 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200246 14382 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
24952706 14055 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197477 14055 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573569 14055 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
162660720 181186 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 181186 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24955189 14049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197443 14049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL572454 14049 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL608097 215835 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
24952353 14051 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197454 14051 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572882 14051 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 164386 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 164386 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11663047 1647 20 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
3501 1647 20 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
CHEMBL204989 1647 20 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
162656670 180918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593612 215812 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
24952708 14045 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197439 14045 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572392 14045 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953057 14073 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197534 14073 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575630 14073 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
24955187 76718 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL206552 76718 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574304 76718 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
15983441 85645 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228411 85645 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145977587 163686 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163686 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL509604 215576 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162668785 182698 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789420 182698 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 211063 7 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162662050 181847 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4778562 181847 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
49798989 14371 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172605 14371 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200194 14371 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799137 14408 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173725 14408 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200304 14408 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
25126427 2141 9 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2141 9 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2141 9 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
45487747 196884 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 196884 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23728637 151722 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151722 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747296 171364 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 171364 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804161 91749 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91749 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10119117 88334 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 88334 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
23627613 196937 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 196937 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596967 196769 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 196769 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 197125 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 197125 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 197308 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 197308 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747294 171067 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 171067 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
155543279 173295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 173295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747247 174054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 174054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45486911 197181 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 197181 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486917 197434 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 197434 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71717140 88328 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 88328 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
142747243 174735 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174735 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747265 175613 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175613 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
44596867 196970 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 196970 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486909 197145 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 197145 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71580034 88335 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 88335 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127070 198560 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 198560 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24803165 88794 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236396 88794 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
142747268 171602 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171602 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
25127070 198560 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 198560 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
155552384 174143 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 174143 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
142747256 175676 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175676 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627556 198477 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 198477 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596965 196838 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 196838 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25124736 198561 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 198561 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71579840 88322 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 88322 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 88318 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 88318 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44597068 196770 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 196770 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44206680 197001 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 197001 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
21023902 3535 28 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3535 28 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3535 28 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
44597069 197484 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 197484 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25126424 197022 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 197022 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71716535 88329 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 88329 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579748 88319 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 88319 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747285 174147 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 174147 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627554 196904 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 196904 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627555 197757 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 197757 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 196951 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 196951 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
16656749 197122 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 197122 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 197164 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 197164 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25128051 197692 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 197692 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 198561 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 198561 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747253 171103 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 171103 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
10173280 2995 51 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2995 51 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2995 51 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
2164 3526 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3526 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3526 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
45486918 197248 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568388 197248 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627492 196857 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 196857 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
71717139 88325 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 88325 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24803990 91795 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL241128 91795 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627612 197812 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 197812 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71719581 88323 0 None 19 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 88323 0 None 19 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127071 198559 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 198559 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
44596965 196838 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 196838 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627305 197433 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 197433 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627251 198919 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 198919 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579743 88314 0 None -43 2 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 88314 0 None -43 2 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720175 88332 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 88332 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24804323 90820 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90820 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597068 196770 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 196770 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 197164 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 197164 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45487731 198563 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 198563 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747289 170591 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170591 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 171386 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 171386 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627722 197204 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 197204 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24803168 89892 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237877 89892 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627249 197234 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 197234 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804816 146393 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 146393 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747251 172491 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 172491 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 173450 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 173450 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597398 196798 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 196798 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
155512483 169665 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169665 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
23627722 197204 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 197204 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125422 197287 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 197287 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
16656749 197122 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 197122 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486908 196892 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 196892 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71718372 88327 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 88327 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
142747255 171441 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 171441 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
10173280 2995 51 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2995 51 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2995 51 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
44597071 198562 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 198562 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
142747273 172077 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 172077 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804324 89894 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89894 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
21023902 3535 28 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3535 28 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3535 28 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
25128051 197692 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 197692 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
71580134 88339 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 88339 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44596967 196769 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 196769 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747298 173255 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 173255 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597070 196773 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 196773 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
10173280 2995 51 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
3516 2995 51 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
CHEMBL567303 2995 51 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
71719581 88323 0 None -19 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 88323 0 None -19 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24893978 1010 9 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 1010 9 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 1010 9 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
25127072 197738 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 197738 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
45487748 197750 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 197750 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596964 196951 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 196951 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 196938 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 196938 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
24804326 145350 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 145350 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597070 196773 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 196773 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
11272107 88313 42 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 88313 42 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24803167 89893 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237878 89893 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
23627430 196893 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566145 196893 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 197125 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 197125 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747254 170506 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 170506 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747238 175534 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 175534 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45487747 196884 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 196884 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 196938 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 196938 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
25127071 198559 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 198559 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25067560 187971 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187971 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
45487731 198563 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 198563 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25127072 197738 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 197738 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24804325 145354 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 145354 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90884 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90884 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
25125422 197287 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 197287 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
71718978 88331 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 88331 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
71580033 88336 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348525 88336 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25125764 197191 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 197191 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 197191 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 197191 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44597071 198562 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 198562 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
71579743 88314 0 None 43 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 88314 0 None 43 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24804491 89954 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89954 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
71719582 88333 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 88333 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579843 88324 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 88324 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
45487748 197750 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 197750 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
10120078 67642 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67642 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448692 94898 2 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94898 2 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
45486916 197243 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568358 197243 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597398 196798 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 196798 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25126424 197022 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 197022 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125075 197737 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 197737 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747291 169900 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169900 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747279 174508 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 174508 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627557 196944 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 196944 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24802993 89250 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236800 89250 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71579744 88315 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 88315 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486910 197376 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 197376 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 197308 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 197308 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579935 88326 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 88326 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
25126427 2141 9 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2141 9 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2141 9 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
21023902 3535 28 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3535 28 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3535 28 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
142747275 169646 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169646 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747242 170535 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 170535 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174965 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174965 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
23627249 197234 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 197234 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597069 197484 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 197484 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23627612 197812 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 197812 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125075 197737 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 197737 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
148470142 169677 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169677 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747258 173814 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173814 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747281 175951 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175951 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44435003 146365 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392142 146365 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71720174 88330 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 88330 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
25067045 155508 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 155508 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL387916 212413 0 None - 0 Rat 8.0 pKd = 8 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
25067560 187971 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187971 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580475 193220 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 193220 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 188018 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 188018 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580519 187884 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187884 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 188338 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 188338 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL389653 212431 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 209446 13 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL389654 212432 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL218698 209398 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist potency against human urotensin-2-induced contraction of rat aortic ringAntagonist potency against human urotensin-2-induced contraction of rat aortic ring
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
2164 3526 17 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3526 17 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3526 17 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
44206682 10478 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL1165145 10478 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 197001 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 197001 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 197001 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 197001 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
46907359 10463 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10463 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
11663047 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
11663047 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
3501 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
3501 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
CHEMBL204989 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
CHEMBL204989 1647 20 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
9441 3956 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27791374
9436 103 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12943190
2163 3452 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
9803617 3452 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
CHEMBL93758 3452 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
10173280 2995 51 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
3516 2995 51 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
CHEMBL567303 2995 51 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
10886 3663 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720777 3663 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720778 3663 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
11438 1486 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
46862051 1486 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
11995575 3961 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
2156 3961 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
CHEMBL437110 3961 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
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ligand		 Fold
selectivity		 # Tested
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 p-value
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Type		 Assay
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CHEMBL3315148 211372 0 None - 1 Rat 10.9 pEC50 = 10.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315144 211368 0 None - 1 Rat 10.7 pEC50 = 10.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315139 211363 9 None - 1 Rat 9.4 pEC50 = 9.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 211376 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 211364 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315146 211370 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 213718 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL437430 213718 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3315150 211374 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137628790 160996 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160996 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160996 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177635 121207 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 121207 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 121207 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 121207 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051713 141028 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 141028 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 209403 0 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630764 161104 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 161104 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 161104 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 161132 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 161132 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 161132 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177633 121205 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 121205 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629788 161180 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 161180 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 161180 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177633 121205 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 121205 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 161166 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 161192 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629789 161181 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 161181 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 161181 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 161166 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
44409478 75937 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205157 75937 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
155519842 170375 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 170375 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
15983315 77345 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL208436 77345 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11640431 141359 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383698 141359 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629655 161166 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 121197 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 121197 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631060 161155 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 161155 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 161155 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 121197 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 121197 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 121199 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 121199 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 121199 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 121199 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
2151 244 9 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
9797568 244 9 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
CHEMBL192359 244 9 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
11626617 77360 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL208536 77360 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
15983313 98260 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL274508 98260 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983200 77358 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL208512 77358 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL3104463 211059 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11684574 166036 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL425592 166036 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104463 211059 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 161202 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 161166 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629651 161161 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 161161 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 161161 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177624 121196 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 121196 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 121196 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 121196 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315149 211373 0 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
15983196 195596 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL555609 195596 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631008 161142 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 161142 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 161142 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
127050201 140939 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140939 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155544020 173315 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 173315 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629875 161191 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 161191 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 161191 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
11325792 140167 9 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
CHEMBL380346 140167 9 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
11559579 74765 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL203106 74765 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
11631605 75055 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL203531 75055 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11546868 75960 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205254 75960 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983325 138706 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377946 138706 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
137631155 161202 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11552098 75009 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203337 75009 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11625650 76764 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206811 76764 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
44409467 74755 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203080 74755 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL572699 74755 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629875 161191 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 161191 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 161191 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127049894 140961 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140961 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137628890 160974 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160974 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160974 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
44409534 75557 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204516 75557 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
11546571 75982 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL205430 75982 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL3104461 211057 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 161202 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 161132 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 161132 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 161132 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104461 211057 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11674961 140348 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL380745 140348 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11508921 77174 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207882 77174 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11569119 76280 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205859 76280 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11566781 76627 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206371 76627 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631154 161201 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11510666 140717 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL381756 140717 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL3315143 211367 0 None - 1 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
121335724 158944 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158944 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
155560750 175081 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 175081 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104460 211056 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11591072 138713 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377973 138713 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983317 75474 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL204227 75474 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
122177634 121206 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 121206 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629651 161161 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 161161 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 161161 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137641820 161226 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 161226 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 161226 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11531958 141298 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383326 141298 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11524599 76727 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206596 76727 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983311 138890 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL378235 138890 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 161192 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155532198 171740 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171740 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2151 244 9 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 244 9 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 244 9 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11532525 76053 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL205735 76053 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11573773 141064 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382477 141064 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
127052350 140998 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140998 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177625 121197 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 121197 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315147 211371 0 None - 1 Rat 8.6 pEC50 = 8.6 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
155537097 172256 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 172256 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104471 211063 7 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177625 121197 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 121197 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104465 211061 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11697064 76737 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206661 76737 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104465 211061 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177629 121201 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 121201 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177629 121201 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 121201 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104464 211060 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11559558 76027 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205628 76027 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
11495815 76728 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206597 76728 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11595438 77661 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL208886 77661 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
137631155 161202 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104464 211060 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155532198 171740 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171740 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137631154 161201 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11681737 75978 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205390 75978 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983323 76747 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206719 76747 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
122177624 121196 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 121196 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 121196 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 121196 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537097 172256 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 172256 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
121335724 158944 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158944 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL3104462 211058 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11526048 74700 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203051 74700 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104462 211058 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
2151 244 9 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 244 9 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 244 9 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
15983321 75533 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204368 75533 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104467 211062 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11627432 75053 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203528 75053 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11501947 76031 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205681 76031 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983198 141287 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL383258 141287 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11648503 76717 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206551 76717 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11609885 141035 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL382401 141035 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL593662 215813 9 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL593662 215813 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630539 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL593662 215813 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137629890 161012 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 161012 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 161012 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631008 161142 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 161142 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 161142 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 161192 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631154 161201 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
135747623 175065 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 175065 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137641820 161226 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 161226 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 161226 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 121206 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 121206 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630539 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 161075 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140948 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140948 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 209403 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
135747623 175065 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 175065 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630689 161099 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 161099 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 161099 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177631 121203 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 121203 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 121203 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 121203 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628790 160996 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160996 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160996 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631060 161155 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 161155 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 161155 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 161021 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 161021 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 161021 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630764 161104 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 161104 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 161104 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127051713 141028 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 141028 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3315141 211365 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
137630124 161048 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 161048 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 161048 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 161192 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 161069 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 161069 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 161069 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
2151 244 9 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 244 9 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 244 9 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11696838 77156 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207823 77156 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL573857 77156 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3315145 211369 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
11537255 74441 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL202725 74441 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11582902 75950 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL205201 75950 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 161192 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104460 211056 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11604535 75998 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205488 75998 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
122177629 121201 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 121201 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628942 160984 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160984 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160984 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630802 161111 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 161111 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 161111 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
137631155 161202 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 161156 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177630 121202 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 121202 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177630 121202 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 121202 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 161166 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155567837 176037 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 176037 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629789 161181 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 161181 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 161181 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 121206 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 121206 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 121206 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 121204 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 121204 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 121204 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 121204 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155524087 170893 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170893 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
122177629 121201 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 121201 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628889 160973 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160973 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160973 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140948 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140948 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177631 121203 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 121203 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 121203 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 121203 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155536007 172126 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 172126 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628942 160984 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160984 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160984 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177636 121208 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 121208 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104644 211069 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104644 211069 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
44409477 77147 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207783 77147 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11496131 140339 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL380704 140339 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
15983319 76772 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL206832 76772 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
122177636 121208 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 121208 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315142 211366 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
137629655 161166 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 161166 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 161166 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 161021 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 161021 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 161021 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630124 161048 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 161048 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 161048 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629788 161180 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 161180 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 161180 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629877 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127051389 140993 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140993 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155529504 171432 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 171432 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155524087 170893 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170893 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218994 209403 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629877 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 161193 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177628 121200 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 121200 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 121200 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 121200 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 172346 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 172346 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177632 121204 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 121204 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 121204 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 121204 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 172346 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 172346 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628889 160973 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160973 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160973 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
44409548 77329 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL208362 77329 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL573837 77329 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 211066 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11525327 141097 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382688 141097 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11653844 75394 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203937 75394 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11524788 76514 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205991 76514 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104637 211064 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155560750 175081 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 175081 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104637 211064 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137628890 160974 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160974 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160974 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 161192 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 161192 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 161192 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 161069 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 161069 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 161069 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631154 161201 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177627 121199 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 121199 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 121199 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 121199 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630802 161111 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 161111 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 161111 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177626 121198 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 121198 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 121198 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 121198 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
11496252 138704 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL377938 138704 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11567714 75151 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203626 75151 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104471 211063 7 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631154 161201 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL3104471 211063 7 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629890 161012 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 161012 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 161012 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177628 121200 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 121200 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 121200 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 121200 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051389 140993 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140993 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
11663047 1647 20 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
3501 1647 20 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
CHEMBL204989 1647 20 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
11589093 75916 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204988 75916 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
122177630 121202 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 121202 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104471 211063 7 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177630 121202 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 121202 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 121208 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 121208 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 121208 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 121208 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631154 161201 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 161201 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 161201 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630689 161099 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 161099 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 161099 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177635 121207 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 121207 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 121205 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 121205 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 121207 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 121207 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 121205 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 121205 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104638 211065 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155544020 173315 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 173315 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104467 211062 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 211065 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
24955187 76718 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL206552 76718 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL574304 76718 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 211066 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
127052350 140998 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140998 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137631155 161202 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 161202 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 161202 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177626 121198 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 121198 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 121198 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 121198 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155529504 171432 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 171432 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
127049894 140961 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140961 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
127050201 140939 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140939 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155520913 170536 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 170536 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44189349 181795 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181795 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104464 211060 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134134886 144470 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3906682 144470 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
134155324 150936 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3957806 150936 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
156012877 177441 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638745 177441 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162657061 180900 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180900 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 211063 7 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156017817 177829 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4643905 177829 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104471 211063 7 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155552384 174143 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 174143 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
134156076 151296 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3960613 151296 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
71579840 88322 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 88322 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86291695 116258 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358677 116258 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
71579744 88315 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 88315 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL437430 213718 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86292101 116266 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358687 116266 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL437430 213718 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134152840 153512 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
CHEMBL3979822 153512 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
10119117 88334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 88334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
156016806 177724 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642313 177724 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71579748 88319 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 88319 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747255 171441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 171441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
123185525 143440 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3898238 143440 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134133034 144539 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3907266 144539 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
86291907 116262 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
CHEMBL3358683 116262 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
142747275 169646 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169646 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747296 171364 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 171364 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747256 175676 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175676 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747281 175951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
156013999 177196 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635150 177196 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162648628 179855 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179855 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
2164 3526 17 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3526 17 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3526 17 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL3104637 211064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580034 88335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 88335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86305736 116249 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358667 116249 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
162671682 182889 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182889 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104637 211064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747285 174147 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 174147 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747265 175613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
71719582 88333 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 88333 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
134156326 154284 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3986509 154284 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104640 211067 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104640 211067 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104471 211063 7 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
86291908 116263 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
CHEMBL3358684 116263 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
162646037 179514 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 179514 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
156014461 177190 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635039 177190 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
142747247 174054 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 174054 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291906 116261 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
CHEMBL3358682 116261 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
86291904 116264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358685 116264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104465 211061 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104465 211061 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580135 88340 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348529 88340 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723010 116252 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358670 116252 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
71719581 88323 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 88323 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723009 116251 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358669 116251 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
11272107 88313 42 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 88313 42 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 88318 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 88318 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747254 170506 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 170506 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 173450 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 173450 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579745 88316 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348504 88316 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134151496 153225 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3977330 153225 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
142747291 169900 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169900 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291696 116259 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358679 116259 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
145966260 164386 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 164386 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
142747243 174735 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174735 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174965 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174965 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL3104463 211059 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71720175 88332 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 88332 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL3104643 211068 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104643 211068 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 211058 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104463 211059 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 211058 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156016802 177720 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642307 177720 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
10173280 2995 51 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2995 51 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2995 51 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
145978068 163736 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163736 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 181293 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 181293 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162660720 181186 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 181186 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579839 88321 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348509 88321 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747279 174508 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 174508 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134148271 149940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3949719 149940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
86291694 116257 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358676 116257 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
142747238 175534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 175534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747253 171103 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 171103 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
71579743 88314 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 88314 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134153111 152561 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
CHEMBL3971737 152561 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
71579843 88324 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 88324 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
86292104 116254 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358672 116254 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
156010342 177073 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4633010 177073 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104459 211055 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104459 211055 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747273 172077 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 172077 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 171386 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 171386 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291905 116265 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358686 116265 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
155512483 169665 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169665 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
162656670 180918 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180918 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579746 88317 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348505 88317 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720174 88330 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 88330 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
118723011 116253 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358671 116253 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104638 211065 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 211065 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
148470142 169677 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169677 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747289 170591 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170591 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
162670598 182922 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182922 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162677235 183495 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 183495 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
123794584 152292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3969435 152292 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134152171 153214 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977271 153214 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3104471 211063 7 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
145977223 163990 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163990 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164729 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164729 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
134133573 143249 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3896625 143249 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
71579935 88326 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 88326 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
71718978 88331 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 88331 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
134141359 146796 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3924660 146796 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
134142270 145625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3915656 145625 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104639 211066 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104639 211066 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747294 171067 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 171067 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
21023902 3535 28 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3535 28 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3535 28 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
142747268 171602 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171602 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104461 211057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86291697 116260 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358680 116260 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3104461 211057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162651887 180271 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 180271 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
86305831 116250 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
CHEMBL3358668 116250 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
142747251 172491 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 172491 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134140417 146279 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3920751 146279 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
71716535 88329 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 88329 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580035 88337 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348526 88337 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134141963 146997 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3926450 146997 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
142747298 173255 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 173255 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579838 88320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348508 88320 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
10303115 10426 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
CHEMBL1163360 10426 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
142747258 173814 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173814 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71717140 88328 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 88328 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
156012366 177407 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638346 177407 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71718372 88327 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 88327 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
134151328 152232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3968841 152232 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
123922871 153286 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977836 153286 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
134146007 148969 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
CHEMBL3942137 148969 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
86294592 116256 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
CHEMBL3358674 116256 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
162668637 182647 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182647 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104644 211069 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
123264706 143361 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3897677 143361 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
71580134 88339 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 88339 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL3104460 211056 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104460 211056 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71717139 88325 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 88325 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580133 88338 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348527 88338 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134142581 145629 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3915670 145629 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
134156353 154362 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3987058 154362 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104467 211062 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104467 211062 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162644923 179429 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 179429 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
155543279 173295 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 173295 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104644 211069 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134151441 153389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3978782 153389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
142747242 170535 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 170535 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
118723012 116255 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358673 116255 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
134138102 147857 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL3933152 147857 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL1165797 208534 0 None - 1 Rat 10.7 pKi = 10.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL577772 215777 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 215777 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1163463 208519 7 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 212437 1 None - 1 Human 9.7 pKi = 9.7 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL390094 212437 1 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL390094 212437 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL390094 212437 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315139 211363 9 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL426020 213343 0 None - 1 Human 9.6 pKi = 9.6 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL426020 213343 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL426020 213343 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL426020 213343 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL218994 209403 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL504097 214174 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44561239 173706 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453587 173706 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL3315142 211366 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44449106 95113 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255509 95113 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
44449079 95463 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
CHEMBL257171 95463 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
44449053 95416 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256989 95416 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL3315141 211365 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315148 211372 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 213718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL437430 213718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL437430 213718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL437430 213718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509604 215576 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL593662 215813 9 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL510618 215585 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2371933 210155 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44449004 95518 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL257415 95518 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL3315147 211371 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL385281 212346 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44448876 95103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255462 95103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL218994 209403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315146 211370 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370836 209932 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2370836 209932 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm0309912
CHEMBL224616 209449 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL388060 212414 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL374468 212201 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CN[C@@H](CC(=O)O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0602110
CHEMBL448403 213956 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155536007 172126 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 172126 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
135747623 175065 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 175065 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3315144 211368 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 211376 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315150 211374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 211364 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
44580517 188019 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497562 188019 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580475 193220 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 193220 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
25067045 155508 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 155508 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL412179 212974 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL389654 212432 0 None 5 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44568398 183534 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479994 183534 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448290 95371 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256773 95371 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
44580679 188001 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497368 188001 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580518 188056 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL497765 188056 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44399254 67636 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190501 67636 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580519 187884 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187884 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 188338 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 188338 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44448714 95508 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257365 95508 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44568339 183849 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480776 183849 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44534500 195006 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
CHEMBL548340 195006 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
25127071 198559 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 198559 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 198561 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 198561 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL509042 215262 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
10120078 67642 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL190533 67642 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL1163479 208525 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46907359 10463 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10463 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
10190075 188758 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL505360 188758 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL3315151 211375 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370837 209933 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2372643 210278 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm0309912
44580564 187803 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495907 187803 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580476 187810 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187810 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
12704866 188338 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 188338 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL387916 212413 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL3315145 211369 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
44597398 196798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 196798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44568429 190765 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL518312 190765 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
10278166 3528 35 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
3531 3528 35 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
CHEMBL1164033 3528 35 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
10120078 67642 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67642 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399063 68629 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191793 68629 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580475 193220 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 193220 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448653 171733 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
CHEMBL446717 171733 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
44561196 173513 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453074 173513 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44593421 186702 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488470 186702 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
23627666 197125 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 197125 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL508811 215140 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44449136 155260 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402813 155260 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44596966 197308 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 197308 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL415851 213205 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0602110
24804491 89954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10210584 184058 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482302 184058 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
45486917 197434 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 197434 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561123 193705 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL527199 193705 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1165794 208532 1 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44597071 198562 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 198562 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568399 192584 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521418 192584 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448469 95196 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL255927 95196 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
25067046 155172 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 155172 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL389653 212431 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL500949 214129 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44596869 196938 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 196938 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
44534506 184053 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482258 184053 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155540766 172508 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4483461 172508 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL425467 213336 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10230399 123352 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL361664 123352 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448314 168755 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
CHEMBL437216 168755 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
44580476 187810 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187810 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448691 94897 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254153 94897 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448337 95246 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256159 95246 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580436 172428 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL447747 172428 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448775 94934 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254356 94934 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561197 173514 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453075 173514 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44448775 94934 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL254356 94934 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44597068 196770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 196770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL3315153 211377 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
24804325 145354 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 145354 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627554 196904 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 196904 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627556 198477 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 198477 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44448691 94897 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254153 94897 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1163471 208521 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
25126424 197022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 197022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 197191 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 197191 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568526 190549 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL517991 190549 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL376223 212243 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501579 214140 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44580563 193137 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522895 193137 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
12052419 68030 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191401 68030 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580473 187938 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187938 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448474 95241 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256140 95241 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448317 95319 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
CHEMBL256516 95319 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
44448514 155443 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403833 155443 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399475 67590 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL190137 67590 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399166 171012 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL445655 171012 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448549 95661 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL258017 95661 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL375241 212215 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44449228 95600 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL257767 95600 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44449107 155205 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL402520 155205 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
155544020 173315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 173315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218825 209401 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)C(C)(C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315149 211373 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL265166 210639 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c([N+](=O)[O-])c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL524855 215622 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL216712 209340 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
155567837 176037 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 176037 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL266651 210690 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44561157 186720 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488642 186720 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
155537736 172346 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 172346 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2164 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL1163475 208523 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
23627305 197433 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 197433 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
2164 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3526 17 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
155550733 174284 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4549818 174284 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
155524911 170918 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4455086 170918 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL505288 214191 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155537097 172256 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 172256 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155560750 175081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 175081 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL219356 209412 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627555 197757 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 197757 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534510 183532 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479993 183532 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155519842 170375 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 170375 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
45487731 198563 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 198563 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44448510 95504 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257337 95504 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580519 187884 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187884 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
44580437 189078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL509831 189078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44561156 186718 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488635 186718 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
2164 3526 17 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3526 17 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3526 17 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399168 135186 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372019 135186 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448431 95548 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257563 95548 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399476 67505 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL189482 67505 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
44399169 135582 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL372911 135582 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399083 160048 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL410825 160048 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399234 161860 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL414847 161860 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580515 188018 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 188018 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44448394 155207 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402543 155207 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580477 188775 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505617 188775 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505358 214192 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
11995575 3961 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
2156 3961 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
CHEMBL437110 3961 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
24804324 89894 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89894 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44596867 196970 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 196970 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486910 197376 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 197376 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561240 172615 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL449192 172615 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
44561238 173510 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453067 173510 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44449052 95415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256988 95415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
10121972 183054 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL479413 183054 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
2164 3526 17 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3526 17 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3526 17 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
155524087 170893 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170893 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155529504 171432 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 171432 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL507406 214310 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
25067045 155508 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 155508 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067560 187971 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187971 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580472 187972 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187972 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
24804323 90820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90884 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90884 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44448513 95145 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255665 95145 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448471 95240 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256138 95240 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448338 95247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256160 95247 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580683 188031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497580 188031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
23627492 196857 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 196857 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
23627613 196937 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 196937 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627557 196944 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 196944 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL264726 96775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580634 187807 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495920 187807 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3526 17 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3526 17 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3526 17 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399453 67826 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190975 67826 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448361 161454 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL412746 161454 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
44448734 169003 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
CHEMBL439244 169003 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
44596965 196838 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 196838 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL264726 96775 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
23627251 198919 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 198919 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 196951 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 196951 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568226 183601 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL480170 183601 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
44568368 184052 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482257 184052 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44568426 191665 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
CHEMBL519629 191665 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
44568484 184007 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481964 184007 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44399062 69391 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193133 69391 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399093 127401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365966 127401 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399084 133615 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL371361 133615 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580472 187972 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187972 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448736 94851 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253749 94851 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448692 94898 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94898 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL439551 213847 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44448732 94822 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253540 94822 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580632 187806 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
CHEMBL495919 187806 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
24863522 188907 10 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL507691 188907 10 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
10173280 2995 51 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2995 51 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2995 51 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
25126427 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
25125422 197287 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 197287 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
24893978 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL1165796 208533 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL218994 209403 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448913 155549 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL404289 155549 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
11691 1979 7 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
3082718 1979 7 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL38576 1979 7 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL218698 209398 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10173280 2995 51 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2995 51 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2995 51 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
10119115 190759 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518301 190759 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
44568428 183600 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480165 183600 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
24804816 146393 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 146393 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
45486909 197145 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 197145 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127072 197738 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 197738 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568370 189838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL516606 189838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
16656749 197122 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 197122 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534490 194973 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
CHEMBL546011 194973 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
155520913 170536 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 170536 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44597070 196773 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 196773 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
23627722 197204 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 197204 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10173280 2995 51 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2995 51 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2995 51 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
44561276 173593 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453329 173593 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448976 95359 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL256721 95359 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
44448947 95459 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL257150 95459 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL223905 209446 13 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 209446 13 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL223905 209446 13 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
21023902 3535 28 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
2165 3535 28 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
CHEMBL522770 3535 28 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
44568369 184054 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482259 184054 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448339 95284 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256365 95284 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580631 187805 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187805 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
44580682 188029 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497579 188029 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
18613636 183893 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL481129 183893 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
12052410 67950 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191110 67950 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052411 69176 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL192552 69176 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052408 126381 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365053 126381 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448656 95028 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254994 95028 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448293 95372 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
CHEMBL256774 95372 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
155560178 174931 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4565187 174931 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
24804326 145350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 145350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
45486911 197181 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 197181 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627612 197812 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 197812 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 197164 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 197164 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127070 198560 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 198560 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
25067046 155172 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL402303 155172 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561237 188245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL499582 188245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448874 95102 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255460 95102 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
44449202 95708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL258251 95708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL3104471 211063 7 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
25067046 155172 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 155172 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580473 187938 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187938 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 188018 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 188018 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
25067046 155172 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 155172 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL452403 213981 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315143 211367 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44534504 183848 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL480775 183848 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL1163477 208524 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
45487747 196884 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 196884 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568400 184003 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481946 184003 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448359 95505 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257349 95505 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580681 188028 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497578 188028 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
25211348 188757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
CHEMBL505353 188757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
44561195 173216 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL452298 173216 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561236 173393 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL452808 173393 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
12052412 69381 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193033 69381 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399398 69400 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
CHEMBL193266 69400 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
44399094 122355 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
CHEMBL359993 122355 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
12052415 135281 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372658 135281 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580631 187805 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187805 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
25067560 187971 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187971 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448428 95144 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255664 95144 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44206680 197001 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 197001 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 197001 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 197001 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
23728637 151722 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151722 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44568427 184025 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482114 184025 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL593662 215813 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448472 155469 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403947 155469 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067045 155508 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 155508 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
45486908 196892 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 196892 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10232516 192548 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521117 192548 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL428990 213489 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(=O)O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627249 197234 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 197234 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804161 91749 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91749 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44448772 155257 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402805 155257 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44448315 95272 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256299 95272 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
44448316 95273 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256300 95273 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448429 155173 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402304 155173 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580633 187630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL494934 187630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580565 193403 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL525759 193403 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
12052413 67513 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL189525 67513 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448733 94850 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253747 94850 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448586 95544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257552 95544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448289 155531 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
CHEMBL404244 155531 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
44580680 188002 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497369 188002 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580630 192745 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522074 192745 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580474 193060 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522381 193060 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448657 95029 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254995 95029 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
44448396 95469 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257187 95469 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44449171 95407 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL256937 95407 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
21023902 3535 28 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3535 28 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3535 28 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
45487748 197750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 197750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
155532198 171740 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171740 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44596967 196769 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 196769 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL383996 212315 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501794 214145 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509009 215242 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL504723 214182 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44597069 197484 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 197484 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568309 191206 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518949 191206 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
11439 3295 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
155817517 3295 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
2161 115 0 None - 1 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
11995575 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
11995575 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2156 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
2156 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
CHEMBL437110 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
CHEMBL437110 3961 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2162 649 0 None - 1 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12770925
2166 3844 0 None - 1 Human 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
24893978 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
8872 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
CHEMBL495075 1010 9 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
9439 907 0 None - 1 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17125276
2151 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
2151 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
9797568 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
9797568 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
CHEMBL192359 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
CHEMBL192359 244 9 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
10278166 3528 35 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
3531 3528 35 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
CHEMBL1164033 3528 35 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
2164 3526 17 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
9846574 3526 17 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
CHEMBL366221 3526 17 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
134813899 2967 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
9438 2967 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
21023902 3535 28 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3535 28 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3535 28 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2167 3948 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14645137
25126427 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
9437 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
CHEMBL567713 2141 9 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
2153 3960 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10499587
2153 3960 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10548501
2153 3960 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10559967
2153 3960 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10581185
10213684 3935 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2152 3935 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
CHEMBL414256 3935 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2160 3042 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
21023902 3535 28 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
21023902 3535 28 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3535 28 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3535 28 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3535 28 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3535 28 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2154 3958 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2154 3958 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3958 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3960 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2153 3960 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2155 3959 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3960 0 None 1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3958 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3959 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2159 761 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12495432