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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]