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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
