Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T43739 | ||||
Target Name | Voltage-gated sodium channel alpha Nav1.8 (SCN10A) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Tetracaine | Drug Info | IC50 = 700 nM | [4] | |
1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | IC50 = 2900 nM | [2] | ||
5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide | Drug Info | IC50 < 30 nM | [3] | ||
N-(2-chlorobenzyl)-5-(4-chlorophenyl)nicotinamide | Drug Info | IC50 = 81 nM | [3] | ||
N-benzyl-5-(4-chlorophenyl)nicotinamide | Drug Info | IC50 = 620 nM | [3] | ||
SCH-725737 | Drug Info | IC50 = 9000 nM | [1] | ||
References | |||||
REF 1 | Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5543-7. | ||||
REF 2 | Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. | ||||
REF 3 | Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. | ||||
REF 4 | Fundamental properties of local anesthetics: half-maximal blocking concentrations for tonic block of Na+ and K+ channels in peripheral nerve. Anesth Analg. 1998 Oct;87(4):885-9. | ||||
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