PHA-709829 [Ligand Id: 3997] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL403858 (PH-709829) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907588] [GtoPdb: 462, 475, 471, 476] [UniProtKB: P02708, P07510, P11230, Q07001] | ||||||||
| ChEMBL | Activity at alpha-1-beta-1-gamma-delta nACh receptor expressed in human TE671 cells by FLIPR assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
| nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| ChEMBL | Activity at alpha-3-beta-4 nACh receptor expressed in human SH-SY5Y cells by FLIPR assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Displacement of [3H]MLA from alpha-7 nACh receptor in human IMR32 cells | B | 8.05 | pKi | 9 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
| ChEMBL | Agonist activity at alpha7-5HT3 chimera expressed in human SH-EP1 cells by FLIPR assay | F | 7.34 | pEC50 | 46 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941] | ||||||||
| ChEMBL | Displacement of [3H]MLA from alpha-7 nACh receptor in rat brain | B | 8.54 | pKi | 2.9 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563] | ||||||||
| ChEMBL | Binding affinity to rat 5HT3 receptor | B | 6.46 | pKi | 350 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3611-3615 [PMID:18490160] |
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]
