Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T10897 | ||||
Target Name | Acyl-CoA desaturase (SCD) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | 2-(4-benzoylpiperazin-1-yl)thiazole-5-carboxamide | Drug Info | IC50 = 2000 nM | [2] | |
CVT-12012 | Drug Info | IC50 = 38 nM | [1] | ||
CVT-12012 | Drug Info | IC50 = 6.1 nM | [1] | ||
MF-152 | Drug Info | IC50 = 106 nM | [4] | ||
MF-152 | Drug Info | IC50 = 2.3 nM | [3] | ||
MF-152 | Drug Info | IC50 = 254 nM | [4] | ||
References | |||||
REF 1 | Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. | ||||
REF 2 | Thiazole analog as stearoyl-CoA desaturase 1 inhibitor. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5214-7. | ||||
REF 3 | Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438). Bioorg Med Chem Lett. 2010 Jan 15;20(2):499-502. | ||||
REF 4 | SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1593-7. | ||||
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