[125I]CGP42112 [Ligand Id: 594] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1885579
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • AT2 receptor in Human [GtoPdb: 35] [UniProtKB: P50052]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
ChEMBL Displacement of [125I]Ang II from AT1 receptor in rat SMC membranes incubated for 60 mins by gamma counting method B 5.77 pKi 1700 nM Ki J Med Chem (2020) 63: 1978-1995 [PMID:32030982]
AT2 receptor in Human [GtoPdb: 35] [UniProtKB: P50052]
GtoPdb - - 10.6 pKd 0.03 nM Kd Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Biochem Biophys Res Commun (1989) 163: 284-91 [PMID:2775266];
Biochem Biophys Res Commun (1991) 181: 1365-71 [PMID:1764088]

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]