<i>N</i>-α-methylhistamine | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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N-α-methylhistamine
Ligand Activity Charts

N-α-methylhistamine [Ligand Id: 1239] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL268490 (Nalpha-Methylhistamine, N-Alpha-Methylhistamine)
H₃ receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] H₃ receptor/Histamine H3 receptor in Mouse [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406] 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
H₃ receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells	B	8.4	pKi	3.98	nM	Ki	Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL	Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay	F	9.4	pEC50	0.4	nM	EC50	Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
H₃ receptor/Histamine H3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
ChEMBL	Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HEK293 cells	B	7.72	pKi	19	nM	Ki	Bioorg. Med. Chem. Lett. (2009) 19: 4075-4078 [PMID:19553110]
GtoPdb	-	-	9	pKi	-	-	-	Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL	Activity at histamine H3 receptor in guinea pig ileum	B	8.6	pKi	2.51	nM	Ki	J. Med. Chem. (2008) 51: 2944-2953 [PMID:18433114]
H₄ receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL	Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2	B	6.5	pKi	316.23	nM	Ki	Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
GtoPdb	-	-	7.2	pKi	-	-	-	J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]
ChEMBL	Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay	F	6.1	pEC50	794.33	nM	EC50	Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]

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]