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Assay Detail

CHEMBL767417

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Binding
Inhibition of Protein kinase C gamma (PKC-gamma)
11
Total Activities
11
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 gamma type (CHEMBL2938)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.
Kuo GH, Prouty C, DeAngelis A, Shen L, O'Neill DJ, Shah C, Connolly PJ, Murray WV, Conway BR, Cheung P, Westover L, Xu JZ, Look RA, Demarest KT, Emanuel S, Middleton SA, Jolliffe L, Beavers MP, Chen X.
J Med Chem (2003) 46 : 4021 -4031
PubMed 12954055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.74 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91829 RUBOXISTAURIN 3.0 1 6.52
CHEMBL340259 INDOLYLYLMALEIMIDE 2 1 5.92
CHEMBL340935 INDOLYLYLMALEIMIDE 1 1 5.87
CHEMBL334555 1 5.57
CHEMBL131035 1 5.56
CHEMBL336179 1 5.48
CHEMBL130774 1 5.29
CHEMBL132223 1 -
CHEMBL340776 1 -
CHEMBL131254 1 -
CHEMBL337642 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91829 RUBOXISTAURIN IC50 = 300.0 nM 6.52
CHEMBL340259 INDOLYLYLMALEIMIDE 2 IC50 = 1200.0 nM 5.92
CHEMBL340935 INDOLYLYLMALEIMIDE 1 IC50 = 1340.0 nM 5.87
CHEMBL334555 IC50 = 2670.0 nM 5.57
CHEMBL131035 IC50 = 2730.0 nM 5.56
CHEMBL336179 IC50 = 3300.0 nM 5.48
CHEMBL130774 IC50 = 5170.0 nM 5.29
CHEMBL132223 IC50 > 10000.0 nM -
CHEMBL340776 IC50 > 10000.0 nM -
CHEMBL131254 IC50 > 10000.0 nM -
CHEMBL337642 IC50 > 10000.0 nM -