A-317920 [Ligand Id: 1216] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL361355 (A-317920)
  • 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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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
GtoPdb - - 7 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]
ChEMBL Binding affinity to human histamine H3 receptor B 7 pKi 100 nM Ki J Med Chem (2011) 54: 26-53 [PMID:21062081]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 7.03 pKi 93.33 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 7.03 pKi 93 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 9.15 pKi 0.71 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 9.15 pKi 0.71 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity to rat cortical histamine H3 receptor B 9.2 pKi 0.63 nM Ki J Med Chem (2011) 54: 26-53 [PMID:21062081]
GtoPdb - - 9.2 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.4 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]

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]