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Assay Detail

CHEMBL768371

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

Binding
Inhibition of bovine protein kinase A (PKA)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

cAMP-dependent protein kinase A (CHEMBL2111446)
Type PROTEIN COMPLEX GROUP
Organism Bos taurus

Publication

Structure-based optimization of novel azepane derivatives as PKB inhibitors.
Breitenlechner CB, Wegge T, Berillon L, Graul K, Marzenell K, Friebe WG, Thomas U, Schumacher R, Huber R, Engh RA, Masjost B.
J Med Chem (2004) 47 : 1375 -1390
PubMed 14998327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202518 1 8.70
CHEMBL3216643 1 8.30
CHEMBL1202525 1 7.41
CHEMBL1204095 1 6.44
CHEMBL1202519 1 6.10
CHEMBL1204097 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202518 IC50 = 2.0 nM 8.70
CHEMBL3216643 IC50 = 5.0 nM 8.30
CHEMBL1202525 IC50 = 39.0 nM 7.41
CHEMBL1204095 IC50 = 360.0 nM 6.44
CHEMBL1202519 IC50 = 800.0 nM 6.10
CHEMBL1204097 IC50 = 45000.0 nM 4.35