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 32:

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]