triprolidine [Ligand Id: 1228] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL855 (Actahist, Actidil, Actifed, Allerfed, Corphed, Histafed, Myfed, Myidyl, Trilitron, Triphed, Triprolidine)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from histamine H1 receptor B 8.8 pKi 1.6 nM Ki J Nat Prod (1993) 56: 441-455 [PMID:8496700]
GtoPdb - - 9 pKi 1 nM Ki Eur J Biochem (1994) 224: 489-95 [PMID:7925364];
J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Potency against histamine H1 receptor on guinea pig ileum B 9.9 pKd 0.13 nM Kd J Med Chem (1995) 38: 3351-3360 [PMID:7650688]
ChEMBL Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min B 8.78 pKi 1.66 nM Ki J Med Chem (1995) 38: 3351-3360 [PMID:7650688]

ChEMBL data shown on this page come from version 33:

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]