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 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]