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 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]
