arpromidine [Ligand Id: 1221] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL293802 (Arpromidine)
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Antagonist activity at histamine H1 receptor against histamine in isolated ileum of guinea pig. F 7.65 pKd 22.39 nM Kd J. Med. Chem. (1989) 32: 1963-1970 [PMID:2569042]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity F 7.65 pKd 22.39 nM Kd J. Med. Chem. (2008) 51: 7193-7204 [PMID:18950149]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity F 8.01 pEC50 9.77 nM EC50 J. Med. Chem. (2008) 51: 7193-7204 [PMID:18950149]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6.5 pKi - - - J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198];
J Pharmacol Exp Ther (2003) 305: 1104-15 [PMID:12626648]
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 8 pKi - - - J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198]

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]