methimepip [Ligand Id: 1254] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL175782 (Methimepip)
  • 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]
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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
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]mepyramine binding to COS-7 cell membranes expressing human histamine H1 receptor B 5 pKi <10000 nM Ki J. Med. Chem. (2005) 48: 2100-2107 [PMID:15771452]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Displacement of [125I]aminopotentidine binding to CHO cell membranes expressing human histamine H2 receptor B 5 pKi <10000 nM Ki J. Med. Chem. (2005) 48: 2100-2107 [PMID:15771452]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
GtoPdb - - 9 pKi 1 nM Ki J Med Chem (2005) 48: 2100-7 [PMID:15771452]
ChEMBL Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptor B 9 pKi 1 nM Ki J. Med. Chem. (2005) 48: 2100-2107 [PMID:15771452]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells B 9 pKi 1 nM Ki J. Med. Chem. (2008) 51: 2944-2953 [PMID:18433114]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor F 9.5 pEC50 0.32 nM EC50 J. Med. Chem. (2005) 48: 2100-2107 [PMID:15771452]
ChEMBL Agonist activity at human histamine H3 receptor assessed as beta galactosidase activity F 9.5 pEC50 0.32 nM EC50 J. Med. Chem. (2008) 51: 2944-2953 [PMID:18433114]
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]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
GtoPdb - - 5.7 pKi - - - J Med Chem (2005) 48: 2100-7 [PMID:15771452]
ChEMBL Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor B 5.7 pKi 1995.26 nM Ki J. Med. Chem. (2005) 48: 2100-2107 [PMID:15771452]
ChEMBL Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 B 5.7 pKi 1995.26 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 5.3 pEC50 5011.87 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]