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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL416477 (A-81988)
  • Angiotensin II type 1a (AT-1a) receptor in Rabbit [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
There should be some charts here, you may need to enable JavaScript!
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
There should be some charts here, you may need to enable JavaScript!
  • AT1 receptor/Type-1B angiotensin II receptor in Rat [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
There should be some charts here, you may need to enable JavaScript!
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]