Target Validation Information
Target ID T10897
Target Name Acyl-CoA desaturase
Target Type
Successful
Drug Potency against Target CVT-12012 Drug Info IC50 = 38 nM [530248]
MF-152 Drug Info IC50 = 254 nM [530690]
CVT-12012 Drug Info IC50 = 6.1 nM [530248]
MF-152 Drug Info IC50 = 106 nM [530690]
2-(4-benzoylpiperazin-1-yl)thiazole-5-carboxamide Drug Info IC50 = 2000 nM [530276]
MF-152 Drug Info IC50 = 2.3 nM [530568]
References
Ref 530248Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. Epub 2009 Jun 13.Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Ref 530690Bioorg Med Chem Lett. 2010 Mar 1;20(5):1593-7. Epub 2010 Jan 21.SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Ref 530248Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. Epub 2009 Jun 13.Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Ref 530690Bioorg Med Chem Lett. 2010 Mar 1;20(5):1593-7. Epub 2010 Jan 21.SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Ref 530276Bioorg Med Chem Lett. 2009 Sep 1;19(17):5214-7. Epub 2009 Jul 9.Thiazole analog as stearoyl-CoA desaturase 1 inhibitor.
Ref 530568Bioorg Med Chem Lett. 2010 Jan 15;20(2):499-502. Epub 2009 Nov 26.Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).

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