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Assay Detail

CHEMBL767445

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of protein kinase C
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Protein kinase C (PKC) (CHEMBL2093867)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Preparation of synthons for the synthesis of protein kinase C inhibitors from rebeccamycin.
Fabre S, Prudhomme M, Rapp M
Bioorg Med Chem Lett (1992) 2 : 449 -452
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.58 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.57
CHEMBL574737 UCN-01 2.0 2 8.39
CHEMBL281948 K-252A 1 7.48
CHEMBL140600 1 7.42
CHEMBL16958 STAUROSPORINONE 1 5.61
CHEMBL423731 1 5.52
CHEMBL127277 1 4.66
CHEMBL268368 STAUROSPORINE AGLYCON 1 4.35
CHEMBL139517 1 -
CHEMBL370100 REBECCAMYCIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 2.7 nM 8.57
CHEMBL574737 UCN-01 IC50 = 4.1 nM 8.39
CHEMBL281948 K-252A IC50 = 33.0 nM 7.48
CHEMBL140600 IC50 = 38.0 nM 7.42
CHEMBL574737 UCN-01 IC50 = 62.0 nM 7.21
CHEMBL16958 STAUROSPORINONE IC50 = 2450.0 nM 5.61
CHEMBL423731 IC50 = 3000.0 nM 5.52
CHEMBL127277 IC50 = 22100.0 nM 4.66
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 44700.0 nM 4.35
CHEMBL139517 IC50 > 50000.0 nM -
CHEMBL370100 REBECCAMYCIN IC50 > 100000.0 nM -