Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T38338 | ||||
Target Name | Voltage-gated calcium channel alpha Cav2.2 (CACNA1B) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Ziconotide | Drug Info | IC50 = 0.005 mcg/ml | [6] | |
Cilnidipine | Drug Info | IC50 = 200 nM | [8] | ||
Ralfinamide | Drug Info | IC50 = 10000 nM | [7] | ||
GNF-PF-3464 | Drug Info | IC50 = 14000 nM | [4] | ||
Hesperidin | Drug Info | IC50 = 9500 nM | [4] | ||
LOMERIZINE | Drug Info | IC50 = 2430 nM | [3] | ||
NSC-180246 | Drug Info | IC50 = 13100 nM | [4] | ||
NSC-87509 | Drug Info | IC50 = 12500 nM | [4] | ||
PD-151307 | Drug Info | IC50 = 320 nM | [2] | ||
PD-157667 | Drug Info | IC50 = 460 nM | [1] | ||
PD-167341 | Drug Info | IC50 = 590 nM | [2] | ||
PD-29361 | Drug Info | IC50 = 4400 nM | [5] | ||
PD-32577 | Drug Info | IC50 = 970 nM | [1] | ||
References | |||||
REF 1 | Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52. | ||||
REF 2 | Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic proper... J Med Chem. 1999 Oct 7;42(20):4239-49. | ||||
REF 3 | Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7. | ||||
REF 4 | In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. | ||||
REF 5 | Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2415-8. | ||||
REF 6 | Bacterial ribosomal subunit assembly is an antibiotic target. Curr Top Med Chem. 2003;3(9):929-47. | ||||
REF 7 | The anti-nociceptive agent ralfinamide inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive Na+ currents in dorsal root ganglion neurons. Eur J Pharmacol. 2005 Mar 14;510(3):197-208. | ||||
REF 8 | Effect of cilnidipine, a novel dihydropyridine Ca++-channel antagonist, on N-type Ca++ channel in rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 1997 Mar;280(3):1184-91. | ||||
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