A331440 [Ligand Id: 4023] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL319000 (A-331440)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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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 Binding affinity of human cortical histamine H1 receptor B 5.72 pKi 1905.46 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3077-3079 [PMID:12372505]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Binding affinity to the human cortical histamine H2 receptor B 5 pKi 10000 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3077-3079 [PMID:12372505]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to histamine H3 receptor B 8.4 pKi 4 nM Ki J. Med. Chem. (2009) 52: 3855-3868 [PMID:19456097]
GtoPdb - - 8.5 pKi - - - Eur J Pharmacol (2004) 487: 183-97 [PMID:15033391]
ChEMBL Binding affinity at human cloned Histamine H3 receptor B 8.56 pKi 2.75 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3077-3079 [PMID:12372505]
ChEMBL Binding affinity to human H3R B 8.7 pKi 2 nM Ki Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Binding affinity at rat cortical Histamine H3 receptor B 7.87 pKi 13.49 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 3077-3079 [PMID:12372505]

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]