azatadine [Ligand Id: 7119] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL946 (Azatadine, Optimine, Trinalin)
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand B 8.41 pKi 3.9 nM Ki J Med Chem (1991) 34: 457-461 [PMID:1671420]
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
ChEMBL Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. F 4.3 pIC50 >50000 nM IC50 J Med Chem (1991) 34: 457-461 [PMID:1671420]

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]