| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T72295 | ||||
| Target Name | PKC-theta messenger RNA (PRKCQ mRNA) | ||||
| Type of Target |
Literature-reported |
||||
| Drug Potency against Target | 4-(1H-indol-5-ylamino)-5-styrylnicotinonitrile | Drug Info | IC50 = 24 nM | [3] | |
| 4-(1H-indol-5-yloxy)-5-styrylnicotinonitrile | Drug Info | IC50 = 690 nM | [3] | ||
| 4-(1H-indol-6-ylamino)-5-styrylnicotinonitrile | Drug Info | IC50 = 1400 nM | [3] | ||
| 4-(3H-indol-4-ylamino)-5-styrylnicotinonitrile | Drug Info | IC50 = 13 nM | [3] | ||
| 8-Octyl-benzolactam-V9 | Drug Info | Ki = 290 nM | [2] | ||
| PROSTRATIN | Drug Info | Ki = 190 nM | [1] | ||
| References | |||||
| REF 1 | A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1. J Med Chem. 1992 May 29;35(11):1978-86. | ||||
| REF 2 | Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta. J Med Chem. 2006 May 4;49(9):2681-8. | ||||
| REF 3 | First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5829-32. | ||||
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