AC-7954 [Ligand Id: 2151] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL192359 (AC-7954)
  • UT receptor/Urotensin II receptor in Human [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
UT receptor/Urotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6]
GtoPdb - - 6.6 pKi - - - J. Med. Chem. (2002) 45: 4950-3 [PMID:12408704];
Bioorg. Med. Chem. (2005) 13: 3057-68 [PMID:15781415]
ChEMBL Activity against human urotensin-2 receptor expressed in NIH3T3 cells B 5.95 pEC50 1122.02 nM EC50 J. Med. Chem. (2006) 49: 2232-2240 [PMID:16570919]
ChEMBL Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay F 5.95 pEC50 1122.02 nM EC50 Bioorg. Med. Chem. (2010) 18: 4844-4854 [PMID:20570157]
ChEMBL Agonist activity for human Urotensin 2 receptor F 6.52 pEC50 300 nM EC50 J. Med. Chem. (2005) 48: 2480-2492 [PMID:15801838]
ChEMBL Agonist activity at human urotensin 2 expressed in CHO cells by FLIPR F 6.6 pEC50 250 nM EC50 J. Med. Chem. (2010) 53: 2695-2708 [PMID:20043680]
ChEMBL Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay F 8.23 pEC50 <=5.95 nM EC50 Bioorg. Med. Chem. (2009) 17: 4657-4665 [PMID:19481466]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]