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, Fenitoina, Hydantol, Lepitoin, NSC-8722, Phentytoin, Phenytek, Phenytex, Phenytoin, Phenytoine, 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 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]
