Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T43739 | Target Info | |||
| Target Name | Voltage-gated sodium channel alpha Nav1.8 (SCN10A) | ||||
| Synonyms |
hPN3; Voltage-gated sodium channel subunit alpha Nav1.8; Sodium channel protein type X subunit alpha; Sodium channel protein type 10 subunit alpha; Peripheral nerve sodium channel 3; PN3
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| Target Type | Successful Target | ||||
| Gene Name | SCN10A | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 3 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 |
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 = 96000 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 ~ 100000 nM
|
[2] | |||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-[3-[2-(Trifluoromethoxy)-5-(trifluoromethyl)phenyl]phenyl]pyrazole-3,5-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1631099; BDBM50332648; 1-(2''-(trifluoromethoxy)-5''-(trifluoromethyl)biphenyl-3-yl)-1H-pyrazole-3,5-dicarboxamide
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| Activity |
IC50 = 1181000 nM
|
[3] | |||
| Compound Name |
1-[3-[2-Fluoro-3-(trifluoromethoxy)phenyl]phenyl]pyrazole-3,5-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1631097; BDBM50332646; 1-(2''-fluoro-3''-(trifluoromethoxy)biphenyl-3-yl)-1H-pyrazole-3,5-dicarboxamide
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| Activity |
IC50 = 1513000 nM
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[3] | |||
| Compound Name |
1-[3-[2,5-Bis(trifluoromethyl)phenyl]phenyl]pyrazole-3,5-dicarboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1631095; BDBM50332645; 1-(2'',5''-bis(trifluoromethyl)biphenyl-3-yl)-1H-pyrazole-3,5-dicarboxamide
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| Activity |
IC50 = 2000000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. | ||||
| REF 2 | 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. | ||||
| REF 3 | Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. | ||||
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