antazoline [Ligand Id: 7116] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1305 (Antazoline, Antaz sulf, Atazoline, Vasocon-a, Vasocon-A)
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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 potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins F 7.14 pKd 72.44 nM Kd Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486]
ChEMBL Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced ileum contraction measured after 15 mins B 7.14 pKd 72.44 nM Kd Eur J Med Chem (2018) 152: 223-234 [PMID:29723785]
ChEMBL Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins B 7.14 pKd 72.44 nM Kd Bioorg Med Chem (2017) 25: 5341-5354 [PMID:28797771]
ChEMBL Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins B 7.14 pKd 72.44 nM Kd Bioorg Med Chem (2019) 27: 1254-1262 [PMID:30792106]

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]