[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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]