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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ligand		 Fold
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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
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Description		 Source

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CHEMBL218994 216182 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 215306 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 215297 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 215298 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 219216 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 215299 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 215313 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 215309 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 188574 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 188574 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 222556 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 222556 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 215307 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 220953 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 215301 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 186869 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 186869 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 220497 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 171195 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 171195 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 171464 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 171464 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 222401 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 222364 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 186293 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 186293 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 215312 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 215310 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 215311 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 217083 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 219137 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 222487 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 217082 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 170880 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 170880 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 188796 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 188796 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 186634 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 186634 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 222593 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 186208 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 186208 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 170515 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 170515 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 171508 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 171508 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 219394 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 220971 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 187476 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 187476 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 20855 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 20855 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 20855 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 189426 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 189426 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 20840 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 20840 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 20840 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 20837 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 20837 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 20837 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 188077 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 188077 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 170769 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 170769 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 7032 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 7032 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 7032 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 92422 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 92422 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 92441 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 92441 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 17616 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 17616 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 21155 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 21155 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 21155 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 170880 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 170880 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 170769 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 170769 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 21138 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 21138 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 21138 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 171195 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 171195 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 222612 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 170465 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 170465 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 20835 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 20835 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 20835 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 170769 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 170769 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 170769 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 170769 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 171195 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 171195 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 20824 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 20824 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 20824 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 92430 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 92430 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 222613 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 170465 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 170465 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 217089 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 146945 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 146945 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 92621 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 92621 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 189051 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 189051 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 21158 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 21158 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 21158 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 168526 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 168526 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 188993 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 188993 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 217842 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 81530 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 81530 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 81530 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 21168 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 21168 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 21168 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 171165 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 171165 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 217088 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 170769 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 170769 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 189668 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 189668 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 144112 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 144112 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 144864 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 144864 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 186846 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 186846 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 170769 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 170769 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 222616 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 92421 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 92421 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 171464 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 171464 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 21142 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 21142 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 21142 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 176172 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 176172 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 189508 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 189508 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 171508 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 171508 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 83502 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 83502 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 170515 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 170515 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 217087 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 21162 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 21162 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 21162 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 20818 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 20818 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 20818 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 92691 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 92691 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 215300 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 217683 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 220137 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 219480 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 220122 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 217081 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 170880 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 170880 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 222615 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 188812 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 188812 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 20825 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 20825 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 20825 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 21127 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 21127 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 21127 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 21136 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 21136 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 21136 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 92647 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 92647 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 189701 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 189701 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 217080 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 21159 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 21159 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 21159 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 190274 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 190274 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 7032 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 7032 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 7032 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 215303 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 21135 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 21135 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 21135 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 171165 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 171165 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 20834 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 20834 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 20834 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 170769 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 170769 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 21169 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 21169 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 21169 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 187317 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 187317 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 21147 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 21147 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 21147 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 92429 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 92429 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 10707 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 10707 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 10707 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 217090 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 170465 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 170465 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 217086 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 215590 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 187679 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 187679 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 216105 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 217842 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 186691 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 186691 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 219149 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 186607 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 186607 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 7032 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 7032 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 7032 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 20816 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 20816 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 20816 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 92595 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 92595 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 215302 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 171508 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 171508 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 20849 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 20849 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 20849 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 83931 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 83931 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 83931 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 171165 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 171165 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 188072 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 188072 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 188570 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 188570 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 171464 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 171464 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 20844 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 20844 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 20844 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 171195 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 171195 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 20819 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 20819 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 20819 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 170769 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 170769 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 170465 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 170465 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 170880 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 170880 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 170515 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 170515 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 20830 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 20830 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 20830 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 215304 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 92620 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 92620 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 171464 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 171464 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 92622 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 92622 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 20832 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 20832 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 20832 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 21175 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 21175 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 21175 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 92431 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 92431 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 222592 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 187050 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 187050 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 186464 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 186464 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 75887 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 75887 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 21106 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 21106 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 21106 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 92432 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 92432 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 143956 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 143956 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 20820 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 20820 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 20820 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 20865 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 20865 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 20865 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 92690 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 92690 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 20831 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 20831 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 20831 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 92630 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 92630 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 144862 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 144862 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 171195 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 171195 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 171508 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 171508 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 220497 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 220760 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 171464 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 171464 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 217085 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 189253 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 189253 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 78091 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 78091 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 21161 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 21161 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 21161 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 84104 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 84104 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 84104 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 21126 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 21126 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 21126 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 148811 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 148811 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 20856 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 20856 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 20856 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 21160 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 21160 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 21160 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 219802 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 170465 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 170465 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 20846 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 20846 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 20846 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 92689 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 92689 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 20828 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 20828 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 20828 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 20838 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 20838 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 20838 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 151395 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 151395 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 148814 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 148814 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 92442 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 92442 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 220924 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 215308 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 170880 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 170880 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 217842 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 222611 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 189048 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 189048 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 170769 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 170769 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 92619 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 92619 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 171464 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 171464 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 142063 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 142063 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 20829 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 20829 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 20829 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 20839 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 20839 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 20839 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 20850 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 20850 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 20850 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 187767 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 187767 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 20822 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 20822 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 20822 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 170880 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 170880 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 21146 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 21146 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 21146 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 21171 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 21171 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 21171 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 170515 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 170515 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 170769 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 170769 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 221919 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 21154 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 21154 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 21154 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 20827 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 20827 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 20827 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 187965 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 187965 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 20821 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 20821 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 20821 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 222614 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 20823 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 20823 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 20823 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 171165 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 171165 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 8428 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 8428 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 8428 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 187697 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 187697 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 222591 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 20817 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 20817 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 20817 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 20845 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 20845 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 20845 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 83493 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 83493 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 83493 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 92420 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 92420 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 170465 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 170465 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 222355 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 189477 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 189477 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 217842 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 188626 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 188626 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 21143 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 21143 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 21143 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 21180 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 21180 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 21180 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 8922 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 8922 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 8922 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 203663 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 203663 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 158501 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 158501 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 178143 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 178143 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 98524 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 98524 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 95109 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 95109 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 203716 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 203716 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 203548 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 203548 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 203904 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 203904 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 204087 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 204087 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 177846 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 177846 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 180074 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 180074 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 180833 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 180833 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 203960 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 203960 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 204213 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 204213 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 95103 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 95103 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 181514 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 181514 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 182392 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 182392 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 203749 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 203749 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 203924 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 203924 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 95110 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 95110 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 205339 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 205339 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 95569 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 95569 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 178381 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 178381 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 205339 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 205339 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 180922 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 180922 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 182455 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 182455 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 205256 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 205256 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 203617 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 203617 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 205340 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 205340 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 95097 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 95097 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 95093 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 95093 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 203549 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 203549 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 203780 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 203780 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 10308 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 10308 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 10308 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 204263 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 204263 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 203801 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 203801 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 95104 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 95104 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 95094 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 95094 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 180926 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 180926 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 203683 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 203683 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 204536 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 204536 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 203730 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 203730 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 203901 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 203901 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 203943 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 203943 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 204471 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 204471 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 205340 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 205340 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 177882 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 177882 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 9769 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 9769 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 9769 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 10299 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 10299 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 10299 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 204027 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 204027 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 203636 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 203636 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 95100 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 95100 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 98570 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 98570 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 204591 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 204591 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 95098 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 95098 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127071 205338 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 205338 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 203617 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 203617 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 204212 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 204212 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 205698 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 205698 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 95089 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 95089 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720175 95107 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 95107 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 97595 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 97595 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 203549 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 203549 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 203943 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 203943 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 205342 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 205342 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 177370 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 177370 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 178165 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 178165 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 203983 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 203983 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 96667 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 96667 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 204013 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 204013 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 153171 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 153171 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 179270 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 179270 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 180229 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 180229 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 203577 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 203577 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 176444 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 176444 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 203983 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 203983 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 204066 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 204066 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 203901 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 203901 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 203671 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 203671 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 95102 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 95102 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 178220 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 178220 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 9769 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 9769 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 9769 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 205341 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 205341 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 178856 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 178856 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 96669 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 96669 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 10308 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 10308 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 10308 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 204471 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 204471 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 95114 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 95114 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 203548 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 203548 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 180034 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 180034 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 203552 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 203552 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 9769 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 9769 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 9769 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 95098 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 95098 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24893978 7797 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 7797 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 7797 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 204517 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 204517 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 204529 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 204529 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 203730 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 203730 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 203717 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 203717 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 152128 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 152128 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 203552 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 203552 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 95088 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 95088 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 96668 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 96668 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 203672 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 203672 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 203904 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 203904 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 177285 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 177285 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579743 95089 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 95089 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747238 182313 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 182313 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 203663 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 203663 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 203717 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 203717 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 205338 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 205338 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 194750 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 194750 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 205342 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 205342 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 204517 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 204517 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 152132 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 152132 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 97659 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 97659 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 204066 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 204066 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 95106 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 95106 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 95111 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 95111 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 203970 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 203970 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 203970 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 203970 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 205341 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 205341 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 95089 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 95089 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24804491 96729 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 96729 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 95108 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 95108 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 95099 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 95099 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 204529 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 204529 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 74416 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 74416 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 101673 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 101673 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
71719581 95098 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 95098 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486916 204022 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 204022 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 203577 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 203577 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 203801 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 203801 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 204516 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 204516 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 176679 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 176679 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 181287 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 181287 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 203723 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 203723 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 96025 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 96025 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 95090 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 95090 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 204155 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 204155 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 204087 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 204087 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 95101 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 95101 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 8922 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 8922 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 8922 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 10308 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 10308 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 10308 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 176425 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 176425 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 177314 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 177314 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 181744 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 181744 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 204013 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 204013 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 204263 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 204263 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 204591 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 204591 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 204516 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 204516 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 176456 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 176456 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 180593 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 180593 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 182730 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 182730 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 153143 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 153143 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 95105 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 95105 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 162287 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 162287 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 219192 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 194750 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 194750 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 199999 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 199999 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 194797 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 194797 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 194663 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 194663 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 195117 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 195117 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 219210 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 216225 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 219211 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 216177 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 10299 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 10299 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 10299 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 17250 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 17250 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 203780 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 203780 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 203780 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 203780 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 17235 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 17235 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 8428 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 8428 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 8428 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 8428 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 8428 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 8428 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 10728 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27791374
9436 6891 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12943190
2163 10225 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 10225 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 10225 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 9769 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 9769 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 9769 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 10435 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 10435 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 10435 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 8268 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 8268 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 10733 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
2156 10733 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
CHEMBL437110 10733 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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CHEMBL3315148 218151 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 218147 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 218142 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 218155 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 218143 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 218149 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 220497 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 220497 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 218153 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 167775 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 167775 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 167775 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 127985 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 127985 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 127985 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 127985 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 147806 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 147806 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 216182 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 167883 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 167883 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 167883 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 167911 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 167911 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 167911 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 127983 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 127983 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 167959 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 167959 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 167959 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 127983 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 127983 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 167945 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 167945 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 167945 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 167971 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 167971 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 167971 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 167960 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 167960 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 167960 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 167945 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 167945 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 167945 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 82712 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 82712 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 177154 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 177154 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 84120 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 84120 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 148137 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 148137 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 167945 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 167945 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 167945 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 127975 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 127975 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 167934 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 167934 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 167934 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 127975 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 127975 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 127977 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 127977 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 127977 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 127977 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 7032 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 7032 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 7032 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 84135 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 84135 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 105036 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 105036 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 84133 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 84133 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 217838 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 172815 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 172815 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 217838 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 167981 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 167981 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 167981 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 167945 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 167945 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 167945 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 167940 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 167940 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 167940 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 127974 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 127974 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 127974 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 127974 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 218152 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 202375 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 202375 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 167921 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 167921 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 167921 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 147717 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 147717 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 180094 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 180094 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 167970 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 167970 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 167970 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 146945 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 146945 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 81540 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 81540 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 81830 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 81830 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 82735 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 82735 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 145484 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 145484 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 167981 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 167981 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 167981 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 81784 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 81784 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 83539 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 83539 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 81530 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 81530 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 81530 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 167970 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 167970 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 167970 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 147739 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 147739 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 167753 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 167753 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 167753 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 82332 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 82332 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 82757 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 82757 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 217836 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 167981 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 167981 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 167981 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 167911 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 167911 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 167911 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 217836 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 147126 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 147126 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 83949 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 83949 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 83055 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 83055 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 83402 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 83402 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 167980 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 167980 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 167980 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 147495 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 147495 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 218146 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 165723 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 165723 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 181860 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 181860 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 217835 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 145491 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 145491 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 82249 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 82249 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 127984 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 127984 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 127984 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 127984 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 167940 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 167940 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 167940 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 168005 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 168005 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 168005 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 148076 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 148076 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 83502 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 83502 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 145668 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 145668 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 167971 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 167971 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 167971 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 178519 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 178519 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 7032 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 7032 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 7032 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 82828 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 82828 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 147842 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 147842 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 147776 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 147776 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 127975 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 127975 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 218150 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 179035 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 179035 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 217842 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 127975 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 127975 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 217840 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 83512 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 83512 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 217840 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 127979 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 127979 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 127979 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 127979 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 217839 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 82802 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 82802 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 83503 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 83503 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 84436 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 84436 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 167981 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 167981 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 167981 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 217839 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 178519 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 178519 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 167980 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 167980 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 167980 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 82753 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 82753 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 83522 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 83522 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 127974 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 127974 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 127974 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 127974 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 179035 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 179035 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 165723 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 165723 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 217837 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 81475 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 81475 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 217837 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 7032 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 7032 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 7032 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 82308 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 82308 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 217841 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 81828 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 81828 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 82806 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 82806 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 148065 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 148065 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 83492 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 83492 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 147813 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 147813 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 222592 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 222592 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 167854 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 167854 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 167854 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 222592 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 167791 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 167791 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 167791 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 167921 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 167921 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 167921 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 167971 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 167971 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 167971 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 167980 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 167980 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 167980 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 181844 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 181844 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 168005 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 168005 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 168005 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 127984 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 127984 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 127984 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 127984 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 167854 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 167854 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 167854 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 147726 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 147726 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 216182 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 181844 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 181844 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 167878 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 167878 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 167878 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 127981 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 127981 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 127981 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 127981 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 167775 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 167775 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 167775 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 167934 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 167934 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 167934 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 167800 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 167800 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 167800 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 167883 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 167883 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 167883 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 147806 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 147806 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 218144 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 167827 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 167827 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 167827 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 167971 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 167971 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 167971 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 167848 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 167848 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 167848 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 7032 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 7032 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 7032 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 83931 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 83931 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 83931 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 218148 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 81216 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 81216 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 82725 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 82725 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 167971 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 167971 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 167971 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 217835 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 82773 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 82773 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 127979 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 127979 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 167763 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 167763 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 167763 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 167890 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 167890 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 167890 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 167981 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 167981 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 167981 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 167935 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 167935 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 167935 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 167935 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 167935 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 167935 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 127980 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 127980 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 127980 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 127980 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 167945 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 167945 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 167945 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 182816 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 182816 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 167960 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 167960 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 167960 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 127984 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 127984 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 127984 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 127984 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 127982 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 127982 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 127982 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 127982 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 177672 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 177672 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 127979 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 127979 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 167752 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 167752 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 167752 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 147726 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 147726 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 127981 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 127981 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 127981 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 127981 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 178905 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 178905 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 167763 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 167763 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 167763 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 127986 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 127986 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 217848 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 217848 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 83922 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 83922 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 147117 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 147117 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 83547 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 83547 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 127986 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 127986 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 218145 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 167945 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 167945 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 167945 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 167800 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 167800 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 167800 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 167827 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 167827 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 167827 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 167959 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 167959 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 167959 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 167972 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 167972 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 167972 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 147771 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 147771 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 178211 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 178211 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 177672 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 177672 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 216182 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 167972 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 167972 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 167972 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 127978 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 127978 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 127978 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 127978 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 179125 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 179125 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 127982 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 127982 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 127982 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 127982 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 179125 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 179125 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 167752 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 167752 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 167752 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 84104 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 84104 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 84104 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 217845 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 147875 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 147875 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 82169 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 82169 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 83289 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 83289 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 217843 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 181860 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 181860 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 217843 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 167753 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 167753 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 167753 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 167971 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 167971 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 167971 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 167848 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 167848 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 167848 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 167980 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 167980 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 167980 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 127977 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 127977 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 127977 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 127977 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 167890 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 167890 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 167890 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 127976 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 127976 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 127976 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 127976 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 145482 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 145482 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 81926 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 81926 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 217842 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 167980 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 167980 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 167980 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 217842 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 167791 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 167791 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 167791 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 127978 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 127978 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 127978 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 127978 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 147771 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 147771 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 8428 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 8428 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 8428 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 82691 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 82691 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 127980 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 127980 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 217842 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 127980 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 127980 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 127986 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 127986 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 127986 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 127986 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 167980 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 167980 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 167980 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 167878 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 167878 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 167878 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 127985 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 127985 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 127983 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 127983 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 127985 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 127985 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 127983 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 127983 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 217844 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 180094 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 180094 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 217841 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 217844 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 83493 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 83493 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 83493 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 217845 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 147776 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 147776 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 167981 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 167981 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 167981 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 127976 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 127976 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 127976 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 127976 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 178211 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 178211 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 147739 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 147739 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 147717 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 147717 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 177315 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 177315 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 188574 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 188574 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 217839 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 151248 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 151248 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 157715 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 157715 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 184220 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 184220 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 187679 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 187679 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 217842 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 184608 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 184608 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 217842 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 180922 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 180922 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 158075 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 158075 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 95097 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 95097 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 123036 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 123036 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 95090 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 95090 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 220497 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 123044 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 123044 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 220497 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 160291 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 160291 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 95109 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 95109 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 184503 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 184503 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 95094 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 95094 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 178220 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 178220 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 150218 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 150218 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 151317 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 151317 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 123040 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 123040 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 176425 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 176425 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 178143 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 178143 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 182455 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 182455 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 182730 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 182730 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 183975 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 183975 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 186634 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 186634 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 10299 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 10299 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 10299 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 217843 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 95110 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 95110 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 123027 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 123027 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 189668 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 189668 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 217843 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 180926 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 180926 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 182392 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 182392 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 95108 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 95108 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 161063 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 161063 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 217846 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 217846 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 217842 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 123041 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 123041 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 186293 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 186293 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 183969 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 183969 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 180833 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 180833 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 123039 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 123039 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 123042 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 123042 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 217840 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 217840 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 95115 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 95115 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 123030 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 123030 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 95098 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 95098 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 123029 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 123029 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 95088 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 95088 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 95093 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 95093 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 177285 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 177285 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 180229 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 180229 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 95091 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 95091 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 160004 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 160004 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 176679 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 176679 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 123037 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 123037 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 171165 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 171165 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 181514 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 181514 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 181744 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 181744 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 217838 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 95107 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 95107 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 217847 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 217847 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 217837 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 217838 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 217837 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 184499 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 184499 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 9769 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 9769 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 9769 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 170515 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 170515 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 188072 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 188072 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 187965 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 187965 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 95096 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 95096 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 181287 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 181287 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 156719 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 156719 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 123035 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 123035 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 182313 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 182313 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 177882 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 177882 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 95089 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 95089 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 159340 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 159340 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 95099 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 95099 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 123032 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 123032 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 183852 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 183852 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 217834 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 217834 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 178856 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 178856 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 178165 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 178165 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 123043 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 123043 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 176444 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 176444 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 187697 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 187697 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 95092 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 95092 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 95105 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 95105 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 123031 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 123031 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 217844 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 217844 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 176456 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 176456 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 177370 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 177370 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 189701 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 189701 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 190274 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 190274 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 159071 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 159071 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 159993 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 159993 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 217842 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 170769 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 170769 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 171508 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 171508 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 150027 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 150027 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 95101 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 95101 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 95106 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 95106 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 153574 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 153574 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 152403 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 152403 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 217845 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 217845 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 177846 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 177846 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 10308 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 10308 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 10308 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 178381 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 178381 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 217836 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 123038 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 123038 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 217836 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 187050 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 187050 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 123028 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 123028 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 179270 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 179270 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 153057 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 153057 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 95104 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 95104 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 95112 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 95112 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 153775 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 153775 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 180034 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 180034 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 95095 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 95095 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 17198 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 17198 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 180593 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 180593 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 95103 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 95103 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 184186 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 184186 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 95102 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 95102 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 159011 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 159011 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 160065 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 160065 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 155748 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 155748 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 123034 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 123034 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 189426 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 189426 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 217848 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 150139 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 150139 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 95114 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 95114 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 217835 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 217835 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 95100 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 95100 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 95113 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 95113 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 152407 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 152407 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 161141 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 161141 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 217841 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 217841 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 186208 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 186208 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 180074 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 180074 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 217848 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 160168 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 160168 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 177314 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 177314 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 123033 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 123033 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 154635 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 154635 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 215313 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 222556 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 222556 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 215298 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 219216 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 219216 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 219216 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 219216 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 218142 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 220122 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 220122 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 220122 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 220122 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 216182 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 220953 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 180485 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 180485 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 218145 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 101888 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 101888 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 102238 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 102238 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 102191 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 102191 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 218144 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 218151 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 220497 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 220497 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 220497 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 220497 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 222355 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 222592 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 222364 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 216934 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 102293 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 102293 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 218150 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 219125 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 101878 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 101878 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 216182 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 218149 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 216711 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 216711 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 216228 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 219193 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 218980 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 220735 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 178905 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 178905 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 181844 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 181844 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 218147 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 218155 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 218153 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 218143 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 194798 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 194798 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 199999 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 199999 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 162287 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 162287 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 219753 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 219211 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 190313 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 190313 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 102146 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 102146 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 194780 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 194780 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 194835 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 194835 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 74410 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 74410 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 194663 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 194663 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 195117 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 195117 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 102283 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 102283 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 190628 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 190628 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 201785 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 201785 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 205338 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 205338 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 205340 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 205340 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 222041 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 74416 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 74416 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 215304 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 17235 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 17235 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 195537 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 195537 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 218154 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 216712 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 217057 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 194582 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 194582 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 194589 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 194589 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 195117 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 195117 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 219192 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 218148 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 203577 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 203577 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 197544 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 197544 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 10301 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 10301 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 10301 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 74416 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 74416 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 75404 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 75404 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 199999 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 199999 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 178512 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 178512 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 180292 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 180292 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 193481 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 193481 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 203904 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 203904 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 221919 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 162039 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 162039 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 204087 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 204087 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 219984 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 96729 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 96729 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 190837 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 190837 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 204213 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 204213 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 200484 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 200484 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 215311 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 205341 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 205341 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 199363 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 199363 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 101971 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 101971 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 161951 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 161951 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 219210 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 220908 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 203717 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 203717 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 190832 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 190832 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 179287 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 179287 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 220115 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 130130 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 130130 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 175534 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 175534 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 194589 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 194589 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 101672 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 101672 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 102021 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 102021 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 179207 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 179207 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 101709 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 101709 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 180293 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 180293 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 101709 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 101709 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 203549 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 203549 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 218156 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 152132 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 152132 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 203683 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 203683 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 205256 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 205256 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 101672 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 101672 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 215300 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 203801 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 203801 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 203970 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 203970 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 197328 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 197328 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 219022 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 220919 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 199916 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 199916 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 10299 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 10299 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 10299 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 74805 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 74805 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 194717 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 194717 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 102016 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 102016 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 102094 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 102094 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 162222 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 162222 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 74364 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 74364 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 177791 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 177791 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 102436 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 102436 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 218994 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 102375 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 102375 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 161984 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 161984 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 180094 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 180094 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 216180 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 218152 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 217418 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 222401 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 216119 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 182816 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 182816 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 217469 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 193499 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 193499 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 179125 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 179125 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 10299 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 10299 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 10299 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 215302 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 204212 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 204212 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 10299 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 10299 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 10299 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 181063 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 181063 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 177697 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 177697 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 220970 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 179035 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 179035 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 181860 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 181860 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 216191 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 204536 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 204536 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 190311 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 190311 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 177154 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 177154 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 205342 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 205342 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 102279 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 102279 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 194663 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 194663 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 195857 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 195857 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 193497 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 193497 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 10299 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 10299 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 10299 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 141964 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 141964 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 102323 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 102323 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 74279 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 74279 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 142360 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 142360 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 166827 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 166827 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 168639 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 168639 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 194797 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 194797 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 161986 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 161986 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 195554 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 195554 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 220971 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 10733 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 10733 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 10733 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 96669 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 96669 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 203749 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 203749 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 204155 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 204155 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 179394 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 179394 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 180289 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 180289 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 102190 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 102190 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 189833 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 189833 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 10299 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 10299 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 10299 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 177672 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 177672 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 178211 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 178211 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 221089 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 162287 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 162287 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 194750 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 194750 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 194751 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 194751 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 97595 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 97595 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 97659 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 97659 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 101920 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 101920 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 102015 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 102015 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 102022 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 102022 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 194810 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 194810 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 203636 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 203636 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 203716 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 203716 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 203723 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 203723 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 103550 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 103550 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 194586 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 194586 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 10299 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 10299 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 10299 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 74601 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 74601 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 168233 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 168233 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 175782 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 175782 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 203617 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 203617 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 103550 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 103550 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 205698 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 205698 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 203730 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 203730 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 190380 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 190380 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 190831 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 190831 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 198444 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 198444 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 190786 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 190786 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 76166 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 76166 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 134179 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 134179 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 140393 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 140393 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 194751 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 194751 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 101626 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 101626 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 101673 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 101673 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 220626 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 101597 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 101597 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 194585 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 194585 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 195686 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 195686 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 9769 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 9769 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 9769 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 8922 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 8922 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 8922 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 204066 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 204066 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 7797 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 7797 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 7797 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 215312 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 216182 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 162328 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 162328 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 8760 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 8760 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 8760 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 216177 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 9769 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 9769 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 9769 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 197538 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 197538 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 190379 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 190379 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 153171 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 153171 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 203924 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 203924 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 204517 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 204517 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 196617 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 196617 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 203901 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 203901 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 201752 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 201752 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 177315 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 177315 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 203552 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 203552 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 203983 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 203983 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 9769 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 9769 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 9769 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 180372 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 180372 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 102134 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 102134 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 102234 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 102234 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 216225 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 216225 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 216225 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 10308 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 10308 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 10308 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 190833 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 190833 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 102059 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 102059 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 194584 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 194584 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 194808 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 194808 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 190672 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 190672 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 74725 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 74725 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 75951 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 75951 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 133159 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 133159 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 101803 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 101803 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 102147 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 102147 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 181710 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 181710 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 152128 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 152128 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 203960 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 203960 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 204591 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 204591 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 203943 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 203943 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 205339 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 205339 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 161951 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 161951 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 195024 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 195024 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 101877 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 101877 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 102483 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 102483 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 217842 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 161951 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 161951 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 194717 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 194717 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 194797 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 194797 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 161951 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 161951 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 220760 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 218146 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 190627 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 190627 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 215303 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 203663 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 203663 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 190782 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 190782 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 102280 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 102280 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 194807 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 194807 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 195536 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 195536 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 179995 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 179995 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 180172 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 180172 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 76156 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 76156 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 76175 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 76175 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 129133 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 129133 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 142059 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 142059 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 194584 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 194584 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 194750 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 194750 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 101919 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 101919 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 203780 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 203780 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 203780 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 203780 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 158501 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 158501 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 190804 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 190804 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 222592 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 162248 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 162248 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 162287 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 162287 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 203671 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 203671 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 199327 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 199327 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 220268 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 204013 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 204013 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 98524 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 98524 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 162036 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 162036 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 102047 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 102047 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 102048 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 102048 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 161952 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 161952 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 194409 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 194409 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 200182 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 200182 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 74287 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 74287 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 101625 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 101625 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 102319 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 102319 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 162310 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 162310 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 194781 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 194781 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 199524 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 199524 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 199839 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 199839 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 101804 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 101804 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 102244 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 102244 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 102182 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 102182 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 10308 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 10308 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 10308 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 204529 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 204529 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 178519 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 178519 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 203548 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 203548 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 219094 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 220924 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 222021 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 220961 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 204263 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 204263 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 197985 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 197985 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 10068 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 10068 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 6903 0 None - 1 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
11995575 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
11995575 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2156 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
2156 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
CHEMBL437110 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
CHEMBL437110 10733 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2162 7436 0 None - 1 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12770925
2166 10616 0 None - 1 Human 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
24893978 7797 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 7797 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 7797 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 7694 0 None - 1 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17125276
2151 7032 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 7032 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 7032 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 7032 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 7032 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 7032 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 10301 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 10301 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 10301 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 10299 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 10299 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 10299 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 9741 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
9438 9741 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
21023902 10308 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 10308 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 10308 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 10720 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14645137
25126427 8922 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 8922 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 8922 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 10731 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10499587
2153 10731 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10548501
2153 10731 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10559967
2153 10731 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10581185
10213684 10707 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2152 10707 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
CHEMBL414256 10707 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2160 9816 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
21023902 10308 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 10308 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 10308 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 10308 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 10308 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 10308 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 10732 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2154 10732 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 10730 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 10732 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 10731 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2153 10731 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 10730 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2155 10730 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 10731 0 None 1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 10730 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 10732 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2159 7548 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12495432