| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T14912 | ||||
| Target Name | Induced myeloid leukemia cell differentiation protein Mcl-1 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | TW-37 | Drug Info | IC50 = 1030 nM | [1] | |
| NSC-180246 | Drug Info | IC50 = 3944.08 nM | [2] | ||
| MORIN | Drug Info | IC50 = 2988.26 nM | [2] | ||
| GNF-PF-5134 | Drug Info | IC50 = 9187.06 nM | [2] | ||
| NSC-66209 | Drug Info | IC50 = 5376.77 nM | [2] | ||
| SULFURETIN | Drug Info | IC50 = 1534.63 nM | [2] | ||
| CEPHALOCHROMIN | Drug Info | IC50 = 1491.9 nM | [2] | ||
| ROSMARINIC ACID | Drug Info | IC50 = 2025.72 nM | [2] | ||
| AMENTOFLAVONE | Drug Info | IC50 = 1634.07 nM | [2] | ||
| GNF-PF-1591 | Drug Info | IC50 = 19733.2 nM | [2] | ||
| BITHIONOL | Drug Info | IC50 = 1898.89 nM | [2] | ||
| QEDIIRNIARHLAQVGDSMDR | Drug Info | IC50 = 52 nM | [1] | ||
| GNF-PF-3955 | Drug Info | IC50 = 3567.91 nM | [2] | ||
| ALTENUSIN | Drug Info | IC50 = 4147.65 nM | [2] | ||
| The Effect of Target Knockout, Knockdown or Genetic Variations | Administration of ABT-737 to Mcl-1 knockout mice induced severe liver apoptosis, suggesting that t uMor-specific inhibition of Mcl-1 is required for therapeutic purposes | [1] | |||
| References | |||||
| REF 1 | J Med Chem. 2006 Oct 19;49(21):6139-42.Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. | ||||
| REF 2 | Bioorg 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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