Target Validation Information
TTD ID T00895
Target Name Protein kinase C epsilon (PRKCE)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 3 nM [2]
LY-317644 Drug Info IC50 = 6400 nM
LY-326449 Drug Info IC50 = 630 nM [4]
RO-316233 Drug Info IC50 = 550 nM [3]
Ro-32-0557 Drug Info IC50 = 48 nM
RO-320432 Drug Info IC50 = 105 nM
[2,2':5',2'']Terthiophen-4-yl-methanol Drug Info IC50 = 3000 nM [1]
[2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde Drug Info IC50 = 700 nM [1]
[2,2':5',2'']Terthiophene-4-carbaldehyde Drug Info IC50 = 5000 nM [1]
References
REF 1 Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.
REF 2 Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 3 Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 4 (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71.

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