[3H](R)-α-methylhistamine [Ligand Id: 1237] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL268229 ((R)-Alpha-Methylhistamine)
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
There should be some charts here, you may need to enable JavaScript!
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 Binding affinity against H1 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (1995) 38: 1593-1599 [PMID:7752184]
ChEMBL Binding affinity to H-1 receptor was determined in guinea pig brain tissue using [3H]- N alpha-methylhistamine ligand B 5 pKi >10000 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 243-248 [PMID:9871662]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
GtoPdb - - 9.2 pKd 0.6 nM Kd Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells B 8.2 pKi 6.31 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor B 8.36 pKi 4.37 nM Ki J. Med. Chem. (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay F 8.57 pKi 2.7 nM Ki J. Med. Chem. (2004) 47: 2833-2838 [PMID:15139761]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells B 8.7 pKi 2 nM Ki J. Med. Chem. (2008) 51: 2944-2953 [PMID:18433114]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHOK1 cells after 2 hrs B 8.96 pKi 1.1 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Inhibition of Histamine H3 receptor B 9.06 pKi 0.88 nM Ki J. Med. Chem. (2003) 46: 1980-1988 [PMID:12723960]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells B 9.1 pKi 0.8 nM Ki Eur. J. Med. Chem. (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL Binding affinity to the human histamine H3 receptor B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2003) 46: 3957-3960 [PMID:12954048]
ChEMBL Displacement of [3H[N-alpha-methylhistamine form human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting B 9.26 pKi 0.55 nM Ki J. Med. Chem. (2010) 53: 3840-3844 [PMID:20384344]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHOK1 cells after 2 hrs B 8.64 pIC50 2.3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting F 8.55 pEC50 2.8 nM EC50 J. Med. Chem. (2010) 53: 3840-3844 [PMID:20384344]
ChEMBL Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor B 9.17 pEC50 0.68 nM EC50 J. Med. Chem. (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 9.5 pEC50 0.32 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Inhibition of rat histamine H3 receptor B 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL pD2 values against H3 receptor of guinea pig jejunum were determined. B 7.8 pKd 15.85 nM Kd J. Med. Chem. (1995) 38: 266-271 [PMID:7830269]
ChEMBL Binding affinity against Histamine H3 receptor B 8.82 pKi 1.5 nM Ki J. Med. Chem. (1995) 38: 1593-1599 [PMID:7752184]
ChEMBL Binding affinity of compound towards Histamine H3 receptor was determined in guinea pig brain tissue using [3H]- N alpha-methylhistamine radioligand B 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 243-248 [PMID:9871662]
ChEMBL Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig ileum LMMP homogenates B 9.82 pKi 0.15 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 1825-1830 [PMID:10406649]
ChEMBL Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenates B 10.07 pKi 0.09 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 1825-1830 [PMID:10406649]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
GtoPdb - - 7.2 pKd - - - Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]
ChEMBL Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 B 6.6 pKi 251.19 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells B 6.74 pKi 184 nM Ki J. Med. Chem. (2008) 51: 3145-3153 [PMID:18459760]
ChEMBL Binding affinity to the human histamine H4 receptor B 6.84 pKi 146 nM Ki J. Med. Chem. (2003) 46: 3957-3960 [PMID:12954048]
ChEMBL Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor B 5.95 pEC50 1122.02 nM EC50 J. Med. Chem. (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 6.2 pEC50 630.96 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]

ChEMBL data shown on this page come from version 28:

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]