Target Validation Information
TTD ID T49368
Target Name PKC-delta messenger RNA (PRKCD mRNA)
Type of Target
Literature-reported
Drug Potency against Target Drug Info Ki = 1.8 nM [1]
8-Octyl-benzolactam-V9 Drug Info Ki = 216 nM [3]
BALANOL Drug Info IC50 = 30 nM
Bisindolylmaleimide-I Drug Info IC50 = 32 nM [4]
Bryostatin-1 Drug Info Ki = 0.44 nM [5]
Diheptan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 529 nM [5]
Dihexan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 915 nM [5]
LY-326449 Drug Info IC50 = 690 nM [6]
PROSTRATIN Drug Info Ki = 190 nM [2]
References
REF 1 Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2561-4.
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.
REF 5 Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C. J Med Chem. 2009 Jul 9;52(13):3969-81.
REF 6 (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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