| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T08074 | ||||
| Target Name | PDK-1 messenger RNA (PDK-1 mRNA) | ||||
| Type of Target |
Literature-reported |
||||
| Drug Potency against Target | (Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one | Drug Info | IC50 = 1800 nM | [2] | |
| BX-201 | Drug Info | IC50 = 18 nM | [2] | ||
| BX-517 | Drug Info | IC50 = 5 nM | [2] | ||
| NU-6102 | Drug Info | IC50 < 500 nM | [1] | ||
| SU-6689 | Drug Info | IC50 = 1100 nM | [2] | ||
| References | |||||
| REF 1 | Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. | ||||
| REF 2 | Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. | ||||
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