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Assay Detail

CHEMBL769112

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Binding
Inhibition of Protein kinase C epsilon
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Protein kinase C epsilon type (CHEMBL3582)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(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.
Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH, Neel DA, Rito CJ, Singh U, Stramm LE, Melikian-Badalian A, Baevsky M, Ballas LM, Hall SE, Winneroski LL, Faul MM.
J Med Chem (1996) 39 : 2664 -2671
PubMed 8709095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.62 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.75
CHEMBL91829 RUBOXISTAURIN 3.0 1 6.22
CHEMBL311543 1 5.96
CHEMBL419866 1 5.42
CHEMBL328229 1 4.24
CHEMBL292495 1 4.10
CHEMBL91959 1 -
CHEMBL315357 1 -
CHEMBL315389 1 -
CHEMBL316239 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 18.0 nM 7.75
CHEMBL91829 RUBOXISTAURIN IC50 = 600.0 nM 6.22
CHEMBL311543 IC50 = 1100.0 nM 5.96
CHEMBL419866 IC50 = 3800.0 nM 5.42
CHEMBL328229 IC50 = 57000.0 nM 4.24
CHEMBL292495 IC50 = 79000.0 nM 4.10
CHEMBL91959 IC50 > 5000.0 nM -
CHEMBL315357 IC50 > 5000.0 nM -
CHEMBL315389 IC50 > 5000.0 nM -
CHEMBL316239 IC50 > 5000.0 nM -