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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