phenytoin [Ligand Id: 2624] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL16 (Dilabid, Dilantin, Dilantin-125, Dilantin-30, Diphenylhydantoin, Epamin, Hydantol, Lepitoin, NSC-8722, Phentytoin, Phenytek, Phenytex, Phenytoin, Phenytoinum, SM-88 COMPONENT PHENYTOIN, Zentropil) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Aldose reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3081] [UniProtKB: P16116] | ||||||||
| ChEMBL | In vitro inhibition of partially purified calf lens aldose reductase | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1988) 31: 230-243 [PMID:3121857] |
| Dihydrofolate reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075051] [UniProtKB: P00376] | ||||||||
| ChEMBL | Inhibition of bovine liver DHFR assessed as NADPH consumption during conversion of dihydrofolic acid to tetrahydrofolic acid | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5644-5647 [PMID:19716698] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| ChEMBL | Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of human cerebellar cortex preparation | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1980) 23: 702-704 [PMID:7392039] |
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-A) receptor of rat ganglion neurons | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1980) 23: 702-704 [PMID:7392039] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of hERG K channel | F | 4 | pIC50 | 100000 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
| Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250] | ||||||||
| ChEMBL | Binding affinity to Nav 1.2 (unknown origin) | B | 4.27 | pKi | 53370 | nM | Ki | Med Chem Res (2013) 22: 3177-3184 |
| ChEMBL | Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2009) 17: 3642-3648 [PMID:19394229] |
| ChEMBL | Inhibition of human NaV1.2 expressed in HEK cells at -60 mV holding potential by patch clamp recording technique | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2010) 18: 7957-7965 [PMID:20943396] |
| GtoPdb | - | - | 4.9 | pIC50 | - | - | - | Mol Pharmacol (1991) 40: 756-65 [PMID:1658608] |
| Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775] | ||||||||
| ChEMBL | Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-clamp technique | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2009) 52: 7528-7536 [PMID:19388676] |
| ChEMBL | Inhibition of rat Nav1.2 expressed in CHL1610 cells at -67 to -107 mV after 2 to 3 mins by whole-cell patch-clamp assay | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2013) 56: 9019-9030 [PMID:24205976] |
| GtoPdb | - | - | 4.7 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1996) 93: 9270-5 [PMID:8799190] |
| Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499] | ||||||||
| ChEMBL | Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells | B | 4.62 | pKi | 24000 | nM | Ki | J Med Chem (2004) 47: 1547-1552 [PMID:14998340] |
| Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858] | ||||||||
| ChEMBL | Inhibition of human voltage-gated sodium channel 1.7 expressed in HEK293 cells assessed as changes in membranre potential after 45 mins by FRET analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 2180-2188 [PMID:22364743] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of human voltage-gated sodium channel 1.5 expressed in HEK293 cells assessed as changes in membranre potential after 45 mins by FRET analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 2180-2188 [PMID:22364743] |
| ChEMBL | Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA | F | 4.31 | pIC50 | 49000 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
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]
