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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