impentamine [Ligand Id: 1252] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL417096 (Impentamine) |
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| 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 | Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor | B | 8.29 | pKi | 5.13 | nM | Ki | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in SK-N-MC cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2006) 49: 2549-2557 [PMID:16610798] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Med Chem (2003) 46: 5445-57 [PMID:14640553] |
| ChEMBL | Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells | F | 8.3 | pEC50 | 5.01 | nM | EC50 | J Med Chem (2006) 49: 2549-2557 [PMID:16610798] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 8.4 | pEC50 | 3.98 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| 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 | 8.63 | pEC50 | 2.34 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | Tested in vitro for antagonist activity against H3 receptor of guinea pig jejunum. | F | 8.4 | pKd | 3.98 | nM | Kd | J Med Chem (1995) 38: 266-271 [PMID:7830269] |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (2006) 49: 2549-2557 [PMID:16610798] |
| 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 | 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 | pEC50 | <10000 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
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]
