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Assay Detail

CHEMBL759069

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

Binding
Inhibition of protein kinase C alpha
10
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 alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety
Jagdmann G, Defauw JM, Lampe JW, Darges JW, Kalter K
Bioorg Med Chem Lett (1996) 6 : 1759 -1764
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.88 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265559 1 7.66
CHEMBL49354 2 7.52
CHEMBL295806 2 7.52
CHEMBL48636 1 7.40
CHEMBL48988 1 6.66
CHEMBL300422 1 6.58
CHEMBL48665 1 5.85
CHEMBL48546 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265559 IC50 = 22.0 nM 7.66
CHEMBL295806 IC50 = 30.0 nM 7.52
CHEMBL49354 IC50 = 30.0 nM 7.52
CHEMBL48636 IC50 = 40.0 nM 7.40
CHEMBL49354 IC50 = 67.0 nM 7.17
CHEMBL295806 IC50 = 160.0 nM 6.80
CHEMBL48988 IC50 = 220.0 nM 6.66
CHEMBL300422 IC50 = 260.0 nM 6.58
CHEMBL48665 IC50 = 1400.0 nM 5.85
CHEMBL48546 IC50 = 2200.0 nM 5.66