Target Validation Information
Target ID T38338
Target Name Voltage-dependent N-type calcium channel
Target Type
Successful
Drug Potency against Target Ziconotide Drug Info IC50 = 0.005 mcg/ml [552342]
NSC-87509 Drug Info IC50 = 12500 nM [531262]
NSC-180246 Drug Info IC50 = 13100 nM [531262]
PD-32577 Drug Info IC50 = 970 nM [525576]
Cilnidipine Drug Info IC50 = 200 nM [553247]
PD-167341 Drug Info IC50 = 590 nM [525605]
LOMERIZINE Drug Info IC50 = 2430 nM [528552]
HESPERIDINE Drug Info IC50 = 9500 nM [531262]
Ralfinamide Drug Info IC50 = 10000 nM [552504]
PD-29361 Drug Info IC50 = 4400 nM [534799]
PD-157667 Drug Info IC50 = 460 nM [525576]
PD-151307 Drug Info IC50 = 320 nM [525605]
GNF-PF-3464 Drug Info IC50 = 14000 nM [531262]
References
Ref 552342Bacterial ribosomal subunit assembly is an antibiotic target. Curr Top Med Chem. 2003;3(9):929-47.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 525576Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Ref 553247Effect 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.
Ref 525605J Med Chem. 1999 Oct 7;42(20):4239-49.Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties.
Ref 528552Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7. Epub 2006 Nov 6.Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 552504The 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 534799Bioorg Med Chem Lett. 1998 Sep 22;8(18):2415-8.Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers.
Ref 525576Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Ref 525605J Med Chem. 1999 Oct 7;42(20):4239-49.Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).

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