A-304121 [Ligand Id: 1258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL302196 (A-304121)
  • 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]
  • Histamine H3 receptor in Guinea pig [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
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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 towards Histamine H1 receptor of human membranes. B 4.16 pKi 69183.1 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2035-2037 [PMID:12113836]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Binding affinity towards Histamine H2 receptor from human membranes B 4.15 pKi 70794.58 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2035-2037 [PMID:12113836]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to human histamine H3 receptor B 6.1 pKi 794.33 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
GtoPdb - - 6.1 pKi - - - J. Pharmacol. Exp. Ther. (2003) 305: 887-96 [PMID:12606603];
Biochem. Pharmacol. (2004) 68: 933-45 [PMID:15294456]
ChEMBL Binding affinity for human histamine H3 receptor on human colon cells B 6.12 pKi 760 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 673-676 [PMID:14741266]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 6.12 pKi 760 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 6.12 pKi 758.58 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 8.6 pKi 2.51 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity to rat cortical histamine H3 receptor B 8.6 pKi 2.51 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
GtoPdb - - 8.6 pKi - - - J. Pharmacol. Exp. Ther. (2003) 305: 887-96 [PMID:12606603];
Biochem. Pharmacol. (2004) 68: 933-45 [PMID:15294456]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 8.6 pKi 2.5 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity towards Histamine H3 receptor of rat cortical membranes. B 8.9 pKi 1.26 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2035-2037 [PMID:12113836]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL Tested in vitro for histamine H3 receptor mediate inhibition of neurogenic contractions in guinea pig isolated ileum assay F 6.98 pKd 104.71 nM Kd Bioorg. Med. Chem. Lett. (2002) 12: 2035-2037 [PMID:12113836]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]