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Assay Detail

CHEMBL767035

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

Binding
Inhibition of Protein kinase C alpha
11
Total Activities
10
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 alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel PKC inhibitory analogs of balanol with replacement of the ester functionality
Erik Jagdmann G, Defauw JM, Lai Y, Crane HM, Hall SE, Buben JA, Hu H, Gosnell PA
Bioorg Med Chem Lett (1995) 5 : 2015 -2020
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.62 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59828 1 7.66
CHEMBL60254 BALANOL 2 7.52
CHEMBL52529 1 7.40
CHEMBL60455 1 7.40
CHEMBL433101 1 6.66
CHEMBL294303 1 6.34
CHEMBL59677 1 6.04
CHEMBL59687 1 5.50
CHEMBL293500 1 4.46
CHEMBL2310935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59828 IC50 = 22.0 nM 7.66
CHEMBL60254 BALANOL IC50 = 30.0 nM 7.52
CHEMBL52529 IC50 = 40.0 nM 7.40
CHEMBL60455 IC50 = 40.0 nM 7.40
CHEMBL60254 BALANOL IC50 = 67.0 nM 7.17
CHEMBL433101 IC50 = 220.0 nM 6.66
CHEMBL294303 IC50 = 460.0 nM 6.34
CHEMBL59677 IC50 = 920.0 nM 6.04
CHEMBL59687 IC50 = 3200.0 nM 5.50
CHEMBL293500 IC50 = 35000.0 nM 4.46
CHEMBL2310935 IC50 > 50000.0 nM -