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Assay Detail

CHEMBL919346

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

Binding
Inhibition of PKBbeta by radiometric filter binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

RAC-beta serine/threonine-protein kinase (CHEMBL2431)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.
Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.
J Med Chem (2007) 50 : 2289 -2292
PubMed 17451235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.44 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226712 1 8.05
CHEMBL228042 1 8.00
CHEMBL228133 1 7.70
CHEMBL227381 1 6.58
CHEMBL389176 1 6.40
CHEMBL227605 1 6.37
CHEMBL104264 1 6.23
CHEMBL375509 1 5.80
CHEMBL227998 1 5.50
CHEMBL376388 1 5.16
CHEMBL227727 1 5.02
CHEMBL389685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226712 IC50 = 9.0 nM 8.05
CHEMBL228042 IC50 = 10.0 nM 8.00
CHEMBL228133 IC50 = 20.0 nM 7.70
CHEMBL227381 IC50 = 260.0 nM 6.58
CHEMBL389176 IC50 = 400.0 nM 6.40
CHEMBL227605 IC50 = 430.0 nM 6.37
CHEMBL104264 IC50 = 590.0 nM 6.23
CHEMBL375509 IC50 = 1600.0 nM 5.80
CHEMBL227998 IC50 = 3200.0 nM 5.50
CHEMBL376388 IC50 = 6900.0 nM 5.16
CHEMBL227727 IC50 = 9500.0 nM 5.02
CHEMBL389685 IC50 > 100000.0 nM -