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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.