Target Validation Information
TTD ID T93262
Target Name PKC-epsilon messenger RNA (PRKCE mRNA)
Type of Target
Literature-reported
Drug Potency against Target 8-Octyl-benzolactam-V9 Drug Info Ki = 510 nM [3]
BALANOL Drug Info IC50 = 50 nM
Bisindolylmaleimide-I Drug Info IC50 = 6 nM [4]
PROSTRATIN Drug Info Ki = 190 nM [2]
RO-316233 Drug Info IC50 = 7516 nM [1]
References
REF 1 Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.
REF 2 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 3 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 4 Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.

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