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Assay Detail

CHEMBL769180

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

Binding
In vitro inhibition of protein kinase C from rat brain.
20
Total Activities
19
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) (CHEMBL2094266)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Indolocarbazole nitrogens linked by three-atom bridges: a potent new class of PKC inhibitors
Vice SF, Bishop W, McCombie SW, Dao H, Frank E, Ganguly AK
Bioorg Med Chem Lett (1994) 4 : 1333 -1338
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.74 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283259 1 8.70
CHEMBL282805 2 8.62
CHEMBL281448 1 8.30
CHEMBL388978 STAUROSPORINE 1 8.22
CHEMBL26872 1 8.15
CHEMBL285613 1 8.00
CHEMBL284632 1 7.96
CHEMBL283903 1 7.85
CHEMBL26817 1 7.82
CHEMBL26074 1 7.77
CHEMBL27387 1 7.72
CHEMBL283399 1 7.70
CHEMBL282298 1 7.70
CHEMBL283930 1 7.62
CHEMBL282612 1 7.62
CHEMBL281948 K-252A 1 7.22
CHEMBL28202 1 7.07
CHEMBL26996 1 7.05
CHEMBL26936 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283259 IC50 = 2.0 nM 8.70
CHEMBL282805 IC50 = 2.4 nM 8.62
CHEMBL281448 IC50 = 5.0 nM 8.30
CHEMBL388978 STAUROSPORINE IC50 = 6.0 nM 8.22
CHEMBL26872 IC50 = 7.0 nM 8.15
CHEMBL285613 IC50 = 10.0 nM 8.00
CHEMBL284632 IC50 = 11.0 nM 7.96
CHEMBL283903 IC50 = 14.0 nM 7.85
CHEMBL26817 IC50 = 15.0 nM 7.82
CHEMBL26074 IC50 = 17.0 nM 7.77
CHEMBL27387 IC50 = 19.0 nM 7.72
CHEMBL283399 IC50 = 20.0 nM 7.70
CHEMBL282298 IC50 = 20.0 nM 7.70
CHEMBL282612 IC50 = 24.0 nM 7.62
CHEMBL283930 IC50 = 24.0 nM 7.62
CHEMBL281948 K-252A IC50 = 60.0 nM 7.22
CHEMBL28202 IC50 = 86.0 nM 7.07
CHEMBL26996 IC50 = 90.0 nM 7.05
CHEMBL282805 IC50 = 120.0 nM 6.92
CHEMBL26936 IC50 = 145.0 nM 6.84