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Assay Detail

CHEMBL822640

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

Binding
Inhibition of c-AMP dependent kinase (PKA) using histone II A protein
12
Total Activities
12
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

Design and synthesis of new leads for PKC bisubstrate inhibitors.
He M, Buisine E, Tartar A, Sergheraert C
Bioorg Med Chem Lett (1994) 4 : 2845 -2850
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.88 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329274 1 5.70
CHEMBL1233654 1 5.52
CHEMBL100102 1 4.30
CHEMBL97026 1 4.00
CHEMBL327291 1 -
CHEMBL97448 1 -
CHEMBL99572 1 -
CHEMBL95737 1 -
CHEMBL318650 1 -
CHEMBL95812 1 -
CHEMBL97796 1 -
CHEMBL97768 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329274 IC50 = 2000.0 nM 5.70
CHEMBL1233654 IC50 = 3000.0 nM 5.52
CHEMBL100102 IC50 = 50000.0 nM 4.30
CHEMBL97026 IC50 = 100000.0 nM 4.00
CHEMBL327291 IC50 = 300000.0 nM -
CHEMBL97448 IC50 > 500000.0 nM -
CHEMBL99572 IC50 = 210000.0 nM -
CHEMBL95737 IC50 = 390000.0 nM -
CHEMBL318650 IC50 = 120000.0 nM -
CHEMBL95812 IC50 = 390000.0 nM -
CHEMBL97796 IC50 = 310000.0 nM -
CHEMBL97768 IC50 = 150000.0 nM -