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Assay Detail

CHEMBL766548

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

Binding
Inhibition of protein kinase C (PKC) isozyme
14
Total Activities
14
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

Indolocarbazoles.3. Synthesis of novel aza analogs of staurosporine and K 252a as PKC inhibitors.
Shankar B, Viet A, Rizvi R, Kirkup M, McCombie S, Ganguly A
Bioorg Med Chem Lett (1994) 4 : 495 -498
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.97 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.10
CHEMBL147986 1 7.55
CHEMBL421947 1 7.30
CHEMBL281948 K-252A 1 7.22
CHEMBL146564 1 7.16
CHEMBL357602 1 6.64
CHEMBL342767 1 6.60
CHEMBL268368 STAUROSPORINE AGLYCON 1 6.26
CHEMBL358130 1 5.92
CHEMBL429225 1 -
CHEMBL358314 1 -
CHEMBL357892 1 -
CHEMBL144479 1 -
CHEMBL144598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 8.0 nM 8.10
CHEMBL147986 IC50 = 28.0 nM 7.55
CHEMBL421947 IC50 = 50.0 nM 7.30
CHEMBL281948 K-252A IC50 = 60.0 nM 7.22
CHEMBL146564 IC50 = 70.0 nM 7.16
CHEMBL357602 IC50 = 230.0 nM 6.64
CHEMBL342767 IC50 = 250.0 nM 6.60
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 550.0 nM 6.26
CHEMBL358130 IC50 = 1200.0 nM 5.92
CHEMBL429225 IC50 ~ 5000.0 nM -
CHEMBL358314 IC50 ~ 5000.0 nM -
CHEMBL357892 IC50 ~ 5000.0 nM -
CHEMBL144479 IC50 ~ 5000.0 nM -
CHEMBL144598 IC50 ~ 5000.0 nM -