Target Poor or Non Binder(s) Information

Target General Information

Target ID

T29678

Target Info

Target Name

Voltage-gated sodium channel alpha Nav1.2 (SCN2A)

Synonyms

Voltage-gated sodium channelsubunit alpha Nav1.2; Sodium channel protein type II subunit alpha; Sodium channel protein brainII subunit alpha; SCN2A; HBSC II

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Target Type

Literature-reported Target

Gene Name

SCN2A

Biochemical Class

Voltage-gated ion channel

UniProt ID

Q99250

Poor Binders of This Target (in total, 11 binders)

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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

Ki = 53370 nM

[1]

Compound Name

Lamotrigine

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Approved

Compound Info

Synonyms

Crisomet; Labileno; Lamictal; Lamictin; Lamiktal; Lamitor; Lamotrigina; Lamotriginum; Desitin Brand of Lamotrigine; Faes Brand of Lamotrigine; Glaxo Wellcome Brand of Lamotrigine; GlaxoSmithKline Brand of Lamotrigine; Juste Brand of Lamotrigine; Lamictal Cd; Lamictal ODT; Lamictal XR; Lamotrigina [Spanish]; Lamotriginum [Latin]; BW 430C; GI 267119X; GW 273293; L 3791; BW-430C; EUR-1048; Lamictal (TN); Lamictin (TN); Lamotrigine [USAN:INN:BAN]; Lamotrigine (JAN/USAN/INN); 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine; 3,5-Diamino-6-(2,3-dichlorophenyl)-as-triazine; 3,5-diamino-6-(2,3-dichlorophenyl)-as-triazine; 6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diamine; 6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diyldiamine; 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

N-(4-Carboxyphenyl)phthalimide

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Investigative

Compound Info

Synonyms

4-(1,3-dioxoisoindol-2-yl)benzoic acid; 4-(1,3-dioxoisoindolin-2-yl)benzoic acid; 4-Phthalimidobenzoic acid; 4-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)benzoic acid; MFCD00023052; 4-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)benzoic acid; MLS-0091937.0001; 4-(1,3-dioxobenzo[c]azolin-2-yl)benzoic acid; ACMC-1ALDL; 4-Phthalimidylbenzoic acid; ChemDiv2_003279; Oprea1_176567; Oprea1_399342; CBDivE_002986; SCHEMBL481667; CHEMBL312097; cid_246499; N-phthaloyl-4-aminobenzoic acid; BDBM45791; CTK4J8862; DTXSID00289176; N-(4-carboxy phenyl) phthalimide; HMS1378F01; ZINC186368; ALBB-030167; NSC59629; 5191AE; NSC-59629; SBB016334; STK257594; AKOS000200541; MCULE-5034800495; 4 N-(4-CARBOXYPHENYL)PHTHALIMIDE; 4-(1,3-dioxo-2-isoindolyl)benzoic acid; AS-64794; DB-052407; BB 0221668; CS-0128346; FT-0629212; ST50327343; C-5398; 4-[1,3-bis(oxidanylidene)isoindol-2-yl]benzoic acid; F0406-3645; 4-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-benz oic acid; 4-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)benzoic acid #; Benzoic acid,4-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-

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Activity

Ki = 50400 nM

[1]

Compound Name

5-(1,3-Dioxoisoindolin-2-yl)-1,3,4-thiadiazole-2-sulfonamide

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Investigative

Compound Info

Synonyms

CHEMBL2298875; BDBM50488724

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Activity

Ki = 61070 nM

[1]

Compound Name

CID 53239561

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Investigative

Compound Info

Synonyms

CHEMBL3236329; SCHEMBL1768494; BDBM50008745

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Activity

IC50 = 65000 nM

[3]

Compound Name

N-(4-Nitrophenyl)phthalimide

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Investigative

Compound Info

Synonyms

2-(4-nitrophenyl)isoindoline-1,3-dione; 2-(4-nitrophenyl)isoindole-1,3-dione; UNII-MJN47DN89K; 1H-Isoindole-1,3(2H)-dione, 2-(4-nitrophenyl)-; MJN47DN89K; CHEMBL27783; 2-(4-Nitrophenyl)-1H-isoindole-1,3(2H)-dione; N-(4-NITROPHENYL)PHTHALAMIDE; NSC406342; NSC 406342; AI3-02623; Oprea1_210160; SCHEMBL1973251; CTK4G7426; DTXSID70185494; ZINC4015298; BDBM50488720; STK390545; AKOS001268560; CCG-233794; MCULE-9891978159; NSC-406342; 2-(4-Nitro-phenyl)-isoindole-1,3-dione; DB-048079; FT-0629238; FT-0629239; ST50170895; 2-(4-nitrophenyl)benzo[c]azolidine-1,3-dione; 1H-Isoindole-1,3(2H)-dione,2-(4-nitrophenyl)-; 2-(4-Nitrophenyl)-1H-isoindole-1,3(2H)-dione #; 2-(4-nitrophenyl)-2,3-dihydro-1H-isoindole-1,3-dione; Z198198220

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Activity

Ki = 65560 nM

[1]

Compound Name

N-[[5-[1-(2-Imidazol-1-ylethyl)indazol-3-yl]-1,2,4-oxadiazol-3-yl]methyl]benzamide

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Investigative

Compound Info

Synonyms

CHEMBL3236343; SCHEMBL1768467; BDBM50008746; N-((5-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indazol-3-yl)-1,2,4-oxadiazol-3-yl)methyl)benzamide; N-[5-[1-[2-(1H-Imidazole-1-yl)ethyl]-1H-indazole-3-yl]-1,2,4-oxadiazole-3-ylmethyl]benzamide

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Activity

IC50 = 71000 nM

[3]

Compound Name

4-(1,3-Dioxoisoindol-2-yl)-2-hydroxybenzoic acid

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Investigative

Compound Info

Synonyms

CHEMBL1972820; 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid; NSC59373; Kinome_2872; Oprea1_011003; Oprea1_057206; CTK1C5227; DTXSID20957789; ZINC241858; BDBM50488717; NSC-59373; STK372166; AKOS000137675; MCULE-4875431601; ST50224253; AB00078796-01; 4-(1,3-dioxoisoindol-2-yl)-2-hydroxy-benzoic acid; 4-(1,3-Dioxoisoindolin-2-yl)-2-hydroxybenzoic acid; 4-(1,3-dioxobenzo[c]azolin-2-yl)-2-hydroxybenzoic acid

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Activity

Ki = 78420 nM

[1]

Compound Name

2-(4-Chlorophenyl)-4(5)-(3-trifluoromethylphenyl)-imidazole

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Investigative

Compound Info

Synonyms

CHEMBL467919; SCHEMBL9048174; BDBM50259540; 2-(4-chlorophenyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazole; 2-(4-chlorophenyl)-5-[3-(trifluoromethyl)phenyl]-1H-imidazole

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

2-(4-Methoxy-2-nitrophenyl)-1H-isoindole-1,3(2H)-dione

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Investigative

Compound Info

Synonyms

CHEMBL2298876; Oprea1_324554; 3-Nitro-4-phthalimidoanisole; CBDivE_002004; ZINC4011829; BDBM50488719; STK368475; AKOS005444327; MCULE-6700436342; SR-01000397373; 2-(4-methoxy-2-nitrophenyl) isoindoline-1,3-dione; SR-01000397373-1; 2-(4-Methoxy-2-nitrophenyl)-1H-isoindole-1,3(2H)-dione #

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Activity

Ki = 108070 nM

[1]

Compound Name

1H-Isoindole-1,3(2H)-dione, 2-(2-nitrophenyl)-

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Investigative

Compound Info

Synonyms

2-(2-nitrophenyl)isoindole-1,3-dione; 2-(2-Nitrophenyl)-1H-isoindole-1,3(2H)-dione; N-(2-Nitrophenyl)phthalimide; CHEMBL97672; NSC406341; NSC 406341; AI3-02612; CBDivE_005823; ARONIS018116; SCHEMBL5846779; CTK1C2862; KS-00004ADH; DTXSID40188013; ZINC3898275; BBL005721; BDBM50488722; MFCD00415667; STK056044; AKOS000485470; MCULE-9025864211; NSC-406341; 2-(2-Nitrophenyl)isoindoline-1,3-dione; ST4035005; H3197; 2-(2-nitrophenyl)benzo[c]azoline-1,3-dione; SR-01000394073; 2-(2-Nitrophenyl)-1H-isoindole-1,3(2H)-dione #; SR-01000394073-1

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Activity

Ki = 133560 nM

[1]

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Non Binders of This Target (in total, 1 non binders)

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Compound Name

N-(2-Carboxyphenyl)Phthalimide

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Investigative

Compound Info

Synonyms

2-(1,3-dioxoisoindol-2-yl)benzoic acid; 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)benzoic acid; N-phthaloylanthranilic acid; 2-(1,3-Dioxoisoindolin-2-yl)benzoic acid; 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-benzoic acid; 2-(1,3-dioxobenzo[c]azolidin-2-yl)benzoic acid; 2-phthalimidobenzoic acid; NSC111178; ACMC-20akct; 2-Phthalimidylbenzoic acid; TimTec1_000752; Oprea1_279984; Oprea1_527124; SCHEMBL481284; CHEMBL419845; CTK1D7614; ZINC61491; 2-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)benzoic acid; DTXSID60296720; HMS1536C04; ALBB-010578; 2950AE; BDBM50488725; MFCD00041218; SBB001039; STK295518; AKOS000151106; MCULE-3020025832; NSC-111178; AS-64793; ST010110; EU-0067309; FT-0629113; R1701; SR-01000393495; SR-01000393495-1; BRD-K49225884-001-01-0; Benzoic acid, 2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-

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Activity

Ki = 337800 nM

[1]

References

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REF 1

Docking, synthesis, and pharmacological evaluation of isoindoline derivatives as anticonvulsant agents. Med Chem Res. 2012 Nov 15;22:3177-84.

REF 2

2,4(5)-diarylimidazoles as inhibitors of hNaV1.2 sodium channels: pharmacological evaluation and structure-property relationships. Bioorg Med Chem. 2009 May 15;17(10):3642-8.

REF 3

Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis. J Med Chem. 2014 Apr 10;57(7):2942-52.

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