methimepip [Ligand Id: 1254] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL175782 (Methimepip) |
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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 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]
