phenytoin [Ligand Id: 2624] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL16 (Dilabid, Hydantol, Phentytoin, Diphenylhydantoin, Dilantin, Phenytoin, Phenytex, NSC-8722, Phenytek, Dilantin-125, SM-88 COMPONENT PHENYTOIN, Dilantin-30)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
  • Nav1.2/Sodium channel protein type II alpha subunit in Rat [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.4/Sodium channel protein type IV alpha subunit in Human [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
There should be some charts here, you may need to enable JavaScript!
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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]