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Assay Detail

CHEMBL919345

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Binding
Inhibition of PKBbeta by radiometric filter binding assay
11
Total Activities
11
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

Identification of inhibitors of protein kinase B using fragment-based lead discovery.
Saxty G, Woodhead SJ, Berdini V, Davies TG, Verdonk ML, Wyatt PG, Boyle RG, Barford D, Downham R, Garrett MD, Carr RA.
J Med Chem (2007) 50 : 2293 -2296
PubMed 17451234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.18 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374742 1 6.70
CHEMBL223339 1 6.55
CHEMBL227029 1 6.29
CHEMBL226870 1 5.52
CHEMBL228224 1 5.28
CHEMBL226766 1 4.92
CHEMBL428462 1 4.75
CHEMBL223393 1 4.51
CHEMBL227924 1 4.47
CHEMBL228114 1 4.10
CHEMBL390066 1 3.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374742 IC50 = 200.0 nM 6.70
CHEMBL223339 IC50 = 280.0 nM 6.55
CHEMBL227029 IC50 = 510.0 nM 6.29
CHEMBL226870 IC50 = 3000.0 nM 5.52
CHEMBL228224 IC50 = 5200.0 nM 5.28
CHEMBL226766 IC50 = 12000.0 nM 4.92
CHEMBL428462 IC50 = 18000.0 nM 4.75
CHEMBL223393 IC50 = 31000.0 nM 4.51
CHEMBL227924 IC50 = 34000.0 nM 4.47
CHEMBL228114 IC50 = 80000.0 nM 4.10
CHEMBL390066 IC50 = 135000.0 nM 3.87