imbutamine [Ligand Id: 1249] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL90019 (Imbutamine) |
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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 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells incubated for 40 mins | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| 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 | 8.39 | pKi | 4.07 | nM | Ki | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | B | 8.39 | pKi | 4.07 | nM | Ki | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | J Med Chem (2003) 46: 5445-57 [PMID:14640553] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in SK-N-MC cells | B | 8.4 | pKi | 3.98 | 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 | 8.4 | pKi | 3.98 | 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 H3 receptor | B | 8.13 | pEC50 | 7.41 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor | B | 8.13 | pEC50 | 7.41 | nM | EC50 | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| 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 | 9.2 | pEC50 | 0.63 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| 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 | 7.7 | pKd | 19.95 | 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 histamine H4 receptor expressed in SK-N-MC cells | B | 7.84 | pKi | 14.45 | nM | Ki | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins | B | 7.9 | pKi | 12.7 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells | B | 8 | pKi | 10 | 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 | 8 | pKi | 10 | 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 | 7.05 | pEC50 | 89.13 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor | B | 7.05 | pEC50 | 89.13 | nM | EC50 | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.5 | pEC50 | 31.62 | 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]
