Target Validation Information
Target ID T49368
Target Name mRNA of PKC-delta
Target Type
Discontinued
Drug Potency against Target LY-326449 Drug Info IC50 = 690 nM [534154]
Dihexan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 915 nM [530134]
GF-109203 Drug Info IC50 = 32 nM [529049]
PROSTRATIN Drug Info Ki = 190 nM [527606]
BALANOL Drug Info IC50 = 30 nM
Bryostatin-1 Drug Info Ki = 0.44 nM [530134]
Diheptan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 529 nM [530134]
Dicarba-Closo-Dodecaborane analogue Drug Info Ki = 1.8 nM [525598]
8-Octyl-benzolactam-V9 Drug Info Ki = 216 nM [528158]
References
Ref 534154J Med Chem. 1996 Jul 5;39(14):2664-71.(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)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 529049J Biol Chem. 2007 Nov 9;282(45):33052-63. Epub 2007 Sep 17.Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
Ref 527606J Med Chem. 1992 May 29;35(11):1978-86.A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 525598Bioorg Med Chem Lett. 1999 Sep 6;9(17):2561-4.Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.
Ref 528158J Med Chem. 2006 May 4;49(9):2681-8.Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.

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