proxyfan [Ligand Id: 1255] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19173 (proxifan, proxyfan) |
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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]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| ChEMBL | Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in CHO-K1 cells | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem (2008) 16: 8729-8736 [PMID:18774720] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - | J Neurochem (2004) 90: 1331-8 [PMID:15341517] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Agonist activity at histamine H3 receptor in rat cortex | F | 8 | pKi | 10 | nM | Ki | J Med Chem (2008) 51: 2944-2953 [PMID:18433114] |
| ChEMBL | PKi was measured by Histamine H3 receptor binding assay (N-alpha-MeHA) on rat cerebral cortex. | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1999) 42: 1193-1202 [PMID:10197963] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - | Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - |
Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells | B | 8.54 | pKi | 2.9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| 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 Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 | B | 7.3 | pKi | 50.12 | 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 | 7.2 | pEC50 | 63.1 | 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]
