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Assay Detail

CHEMBL772605

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

Binding
Inhibition of protein kinase A
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

cAMP-dependent protein kinase (PKA) (CHEMBL2094138)
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 7 5.89 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.09
CHEMBL574737 UCN-01 2.0 2 7.38
CHEMBL16958 STAUROSPORINONE 1 4.59
CHEMBL127277 1 4.47
CHEMBL268368 STAUROSPORINE AGLYCON 1 4.22
CHEMBL139517 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 8.2 nM 8.09
CHEMBL574737 UCN-01 IC50 = 42.0 nM 7.38
CHEMBL574737 UCN-01 IC50 = 250.0 nM 6.60
CHEMBL16958 STAUROSPORINONE IC50 = 25700.0 nM 4.59
CHEMBL127277 IC50 = 34000.0 nM 4.47
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 60000.0 nM 4.22
CHEMBL139517 IC50 > 100000.0 nM -