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 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]