| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T43739 | ||||
| Target Name | Voltage-gated sodium channel subunit alpha Nav1.8 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | N-(2-chlorobenzyl)-5-(4-chlorophenyl)nicotinamide | Drug Info | IC50 = 81 nM | [531169] | |
| Tetracaine | Drug Info | IC50 = 700 nM | [553280] | ||
| SCH-725737 | Drug Info | IC50 = 9000 nM | [529019] | ||
| 5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide | Drug Info | IC50 < 30 nM | [531169] | ||
| N-benzyl-5-(4-chlorophenyl)nicotinamide | Drug Info | IC50 = 620 nM | [531169] | ||
| 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | IC50 = 2900 nM | [529491] | ||
| References | |||||
| Ref 531169 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. Epub 2010 Sep 18.Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. | ||||
| Ref 553280 | 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. | ||||
| Ref 529019 | Bioorg Med Chem Lett. 2007 Oct 15;17(20):5543-7. Epub 2007 Aug 16.Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis. | ||||
| Ref 531169 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. Epub 2010 Sep 18.Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. | ||||
| Ref 531169 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. Epub 2010 Sep 18.Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. | ||||
| Ref 529491 | Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. Epub 2008 May 6.Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.