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

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ChEMBL ligand: CHEMBL268229 ((R)-Alpha-Methylhistamine)
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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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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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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 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 Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay B 7.2 pKi 63.1 nM Ki J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay B 8.2 pKi 6.31 nM Ki J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
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 H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method F 7.4 pEC50 40 nM EC50 Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981]
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 33:

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]