[3H]A81988 [Ligand Id: 3938] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL416477 (A-81988)
  • Angiotensin II type 1a (AT-1a) receptor in Rabbit [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
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  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • AT1 receptor/Type-1B angiotensin II receptor in Rat [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
ChEMBL Compound was evaluated for in vitro potency against angiotensin II receptor, type 1 in isolated rabbit aorta; value ranges from 10.1-10.7 B 10.1 pKd 0.08 nM Kd J Med Chem (1992) 35: 3714-3717 [PMID:1433184]
ChEMBL Antagonist activity at angiotensin AT1 receptor in rabbit aorta F 10.1 pKd 0.08 nM Kd Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL pA2 value determined in vitro against angiotensin II receptor, type 1 using rabbit aortic rings B 10.3 pKd 0.05 nM Kd Bioorg Med Chem Lett (1994) 4: 173-176
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
GtoPdb - - 9.24 pKd 0.57 nM Kd Eur J Pharmacol (1994) 267: 49-54 [PMID:8206129]
ChEMBL Binding affinity against angiotensin II receptor from rat liver B 9.21 pKi 0.61 nM Ki J Med Chem (1993) 36: 2676-2688 [PMID:8410980]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
GtoPdb - - 9.24 pKd 0.57 nM Kd Eur J Pharmacol (1994) 267: 49-54 [PMID:8206129]
ChEMBL Compound was evaluated for binding affinity against angiotensin II receptor, type 1 in rat liver B 9.12 pKi 0.76 nM Ki J Med Chem (1992) 35: 3714-3717 [PMID:1433184]

ChEMBL data shown on this page come from version 32:

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]