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Assay Detail

CHEMBL766409

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

Binding
Inhibition of Protein kinase B alpha
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.68 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202518 1 8.40
CHEMBL3216643 1 8.30
CHEMBL1204095 1 6.80
CHEMBL1202525 1 6.45
CHEMBL1202519 1 5.52
CHEMBL1204097 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202518 IC50 = 4.0 nM 8.40
CHEMBL3216643 IC50 = 5.0 nM 8.30
CHEMBL1204095 IC50 = 160.0 nM 6.80
CHEMBL1202525 IC50 = 355.0 nM 6.45
CHEMBL1202519 IC50 = 3000.0 nM 5.52
CHEMBL1204097 IC50 = 25000.0 nM 4.60