Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
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| Target ID | T12119 | Target Info | |||
| Target Name | Voltage-gated sodium channel alpha Nav1.7 (SCN9A) | ||||
| Synonyms |
hNE-Na; Voltage-gated sodium channel subunit alpha Nav1.7; Sodium channel proteintype IX subunit alpha; Sodium channel proteintype 9 subunit alpha; Sodium channel protein type IX subunit alpha; Sodium channel protein type 9 subunit alpha; Peripheral sodium channel 1; PN1; Neuroendocrine sodium channel; NENA
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| Target Type | Clinical trial Target | ||||
| Gene Name | SCN9A | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Mexiletine
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Approved | Compound Info | ||
| Synonyms |
Mexiletene; Mexiletina; Mexiletinum; Mexilitine; Mexityl; Mexiletine HCL; KO1173; KO-1173; KOE-1173; Mexiletina [INN-Spanish]; Mexiletine (INN); Mexiletine [INN:BAN]; Mexiletinum [INN-Latin]; Mexitil (TN); (+-)-1-(2,6-dimethylphenoxy)propan-2-amine; (2RS)-1-(2,6-dimethylphenoxy)-2-aminopropane; 1-(2',6'-Dimethylphenoxy)-2-aminopropane; 1-(2,6-Dimethylphenoxy)-2-propanamine; 1-(2,6-dimethylphenoxy)propan-2-amine; 1-Methyl-2-(2,6-xylyloxy)ethylamine; 1-methyl-2-(2,6-xylyloxy)ethanamine; 2-(2-Aminopropoxy)-1,3-DiMethyl-Benzene Hydrochloride; 2-(2-aminopropoxy)-1,3-dimethylbenzene
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| Activity |
IC50 = 56000 nM
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[1] | |||
| Compound Name |
Phenytoin
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Approved | Compound Info | ||
| Synonyms |
Aleviatin; Antisacer; Auranile; Causoin; Citrullamon; Citrulliamon; Comital; Comitoina; Convul; Danten; Dantinal; Dantoinal; Dantoine; Denyl; Difenilhidantoina; Difenin; Difetoin; Difhydan; Dihycon; Dihydantoin; Dilabid; Dilantin; Dilantine; Dillantin; Dintoin; Dintoina; Diphantoin; Diphedal; Diphedan; Diphenat; Diphenin; Diphenine; Diphentoin; Diphentyn; Diphenylan; Diphenylhydantoin; Diphenylhydantoine; Diphenylhydatanoin; Ditoinate; Ekko; Elepsindon; Enkelfel; Epamin; Epanutin; Epelin; Epifenyl; Epihydan; Epilantin; Epinat; Epised; Eptal; Eptoin; Fenitoin; Fenitoina; Fentoin; Fenylepsin; Fenytoine; Hidan; Hidantal; Hidantilo; Hidantina; Hidantomin; Hindatal; Hydantal; Hydantin; Hydantoinal; Hydantol; Idantoil; Idantoin; Iphenylhydantoin; Kessodanten; Labopal; Lehydan; Lepitoin; Lepsin; Minetoin; Neosidantoina; Novantoina; Novophenytoin; Oxylan; PHENYTEK; Phanantin; Phanatine; Phenatine; Phenatoine; Phenhydan; Phenhydanin; Phenitoin; Phentoin; Phentytoin; Phenytex; Phenytoine; Phenytoinum; Ritmenal; Saceril; Sanepil; Silantin; Sinergina; Sodanthon; Sodantoin; Sodanton; Solantin; Solantoin; Solantyl; Sylantoic;TOIN; Tacosal; Thilophenyl; Zentronal; Zentropil; Component of Mebroin; Dantoinal klinos; Difenilhidantoina [Spanish]; Dihydan toin; Dilantin acid; Diphenylhydantoine [French]; Ekko capsules; Elepsi ndon; Epdantoin Simple; Epdantoine simple; Epilan D; Extended Phenytoin Sodium; Fen toin; Fenantoin Mn Pharma; Fenidantoin s; Fenytoin Dak; Hidantina senosian; Hidantina vitoria; Ictalis simp le; Ictalis simple; Om hidantoina simple; Phenat ine; Phenytoin AWD; Sodium Diphenylhydantoinate; Taco sal; Toin unicelles; CL12003; D 4007; D4007_SIGMA; Didan TDC 250; Epasmir 5; IFLab1_000214; DILANTIN-30; DPH (VAN); Di-Hydan; Di-Lan; Di-Phetine; Dilantin (TN); Dilantin Infatabs (TN); Dilantin Kapseals (TN); Dilantin-125; Diphenylhydantoin (VAN); Epanutin (TN); Epasmir (5); Epilan-D; Eptoin (TN); Fenidantoin (s); Fenitoina [INN-Spanish]; Neos-Hidantoina; Om-Hydantoine; PHENYTOIN SODIUM, EXTENDED; Phenytek (TN); Phenytoin (PHN); Phenytoin-Gerot; Phenytoine [INN-French]; Phenytoinum [INN-Latin]; Di-Lan (VAN); Didan-tdc-250; Gerot-epilan-D; PHENYTOIN (5,5-DIPHENYLHYDANTOIN); Phenytoin (JP15/USP/INN); Phenytoin [USAN:INN:BAN:JAN]; Hydantoin, 5,5-diphenyl-(8CI); 2,4-Imidazolidinedione, 5,5-diphenyl-(9CI); 2-hydroxy-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one; 5,5-DIPHENYLHYDANTOIN; 5,5-Diphenyl-2,4-imidazolidinedione; 5,5-Diphenyl-imidazolidine-2,4-dione; 5,5-Diphenylhydantoin (IUPAC); 5,5-Diphenylhydantoin (phenytoin); 5,5-Diphenylimidazolidin-2,4-dione; 5,5-Dwufenylohydantoina; 5,5-Dwufenylohydantoina [Polish]; 5,5-diphenylimidazolidine-2,4-dione
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
Safinamide
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Approved | Compound Info | ||
| Synonyms |
133865-89-1; Xadago; (S)-2-((4-((3-Fluorobenzyl)oxy)benzyl)amino)propanamide; Fce-26743; UNII-90ENL74SIG; (2S)-2-[[4-[(3-Fluorophenyl)methoxy]phenyl]methylamino]propanamide; EMD 1195686; 90ENL74SIG; CHEMBL396778; EMD-1195686; AK-77847; 2(s)-(4-(3-fluorobenzyloxy)benzylamino)propionamide; CHEMBL48582; Safinamide [USAN:INN]; 2-(4-(3-Fluorobenzyloxy)benzylamino)propionamide; AC1L2ZLK; Safinamide (USAN/INN); (S)-2-(((4-((3-Fluorophenyl)methoxy)phenyl)methyl)amino)propanamide; EC 603-772-2; SCHEMBL69350; Fce 26743; ON 019190.Na
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| Activity |
IC50 = 100000 nM
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[3] | |||
| Compound Name |
4-[4-Chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-cyano-N-[5-(trifluoromethyl)pyrimidin-2-yl]benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325235; SCHEMBL16531797; BDBM50489963
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| Activity |
IC50 = 51003.5 nM
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[4] | |||
| Compound Name |
3-Cyano-N-(5-fluoropyridin-2-yl)-4-[4-[(1,3,5-trimethylpyrazol-4-yl)methyl]phenoxy]benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325236; SCHEMBL16531503; BDBM50489858
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| Activity |
IC50 = 54000.78 nM
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[4] | |||
| Compound Name |
N-(5-Chloro-6-(3,4-dichlorobenzyloxy)benzo[d]isoxazol-3-yl)methanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3922136; SCHEMBL16061858; BDBM253039; US9493429, 26; N-[5-chloro-6-[(3,4-dichlorophenyl)methoxy]-1,2-benzoxazol-3-yl]methanesulfonamide
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| Activity |
IC50 = 74000 nM
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[5] | |||
| Compound Name |
N-[5-Chloro-6-[[3-chloro-4-(2-methylpropoxy)phenoxy]methyl]-1,2-benzoxazol-3-yl]methanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3897960; SCHEMBL16060022; BDBM253035; US9493429, 10
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| Activity |
IC50 = 86000 nM
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[5] | |||
| Compound Name |
[2-(4-Tert-Butyl-benzyloxy)-3-methoxy-phenyl]-pyrrolidin-1-yl-methanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL194491; BDBM50166798
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| Activity |
IC50 = 90000 nM
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[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J Med Chem. 2011 Jul 14;54(13):4427-45. | ||||
| REF 2 | Asymmetric synthesis and evaluation of a hydroxyphenylamide voltage-gated sodium channel blocker in human prostate cancer xenografts. Bioorg Med Chem. 2012 Mar 15;20(6):2180-8. | ||||
| REF 3 | Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities. J Med Chem. 2010 May 13;53(9):3756-71. | ||||
| REF 4 | QSAR investigation of NaV1.7 active compounds using the SVM/Signature approach and the Bioclipse Modeling platform. Bioorg Med Chem Lett. 2013 Jan 1;23(1):261-3. | ||||
| REF 5 | US patent application no. 9493429B2, Substituted benzoxazoles and methods of use thereof | ||||
| REF 6 | Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2943-7. | ||||
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