| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T93262 | ||||
| Target Name | mRNA of PKC-epsilon | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | BALANOL | Drug Info | IC50 = 50 nM | ||
| 8-Octyl-benzolactam-V9 | Drug Info | Ki = 510 nM | [1] | ||
| PROSTRATIN | Drug Info | Ki = 190 nM | [2] | ||
| GF-109203 | Drug Info | IC50 = 6 nM | [3] | ||
| RO-316233 | Drug Info | IC50 = 7516 nM | [4] | ||
| References | |||||
| REF 1 | J 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. | ||||
| REF 2 | J 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 3 | J 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 4 | Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. | ||||
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