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 (2009) 17: 4657-4665 [PMID:19481466]
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 data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]