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Assay Detail

CHEMBL766360

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Binding
Inhibition of Protein kinase C epsilon
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.
Zhang HC, White KB, Ye H, McComsey DF, Derian CK, Addo MF, Andrade-Gordon P, Eckardt AJ, Conway BR, Westover L, Xu JZ, Look R, Demarest KT, Emanuel S, Maryanoff BE.
Bioorg Med Chem Lett (2003) 13 : 3049 -3053
PubMed 12941331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.89 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 7.92
CHEMBL103055 1 7.12
CHEMBL106384 1 7.10
CHEMBL103628 1 6.77
CHEMBL106061 1 6.60
CHEMBL103506 1 6.51
CHEMBL105477 1 6.21
CHEMBL321315 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 12.0 nM 7.92
CHEMBL103055 IC50 = 75.0 nM 7.12
CHEMBL106384 IC50 = 80.0 nM 7.10
CHEMBL103628 IC50 = 170.0 nM 6.77
CHEMBL106061 IC50 = 250.0 nM 6.60
CHEMBL103506 IC50 = 310.0 nM 6.51
CHEMBL105477 IC50 = 610.0 nM 6.21
CHEMBL321315 IC50 - nM -