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Assay Detail

CHEMBL861331

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

Functional
Inhibition of GSK3 phosphorylation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Zhu GD, Gong J, Claiborne A, Woods KW, Gandhi VB, Thomas S, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Stoll VS, De Jong R, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL.
Bioorg Med Chem Lett (2006) 16 : 3150 -3155
PubMed 16603355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.79 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210390 1 6.03
CHEMBL383264 1 5.82
CHEMBL378963 1 5.52
CHEMBL210246 1 -
CHEMBL207544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210390 IC50 = 930.0 nM 6.03
CHEMBL383264 IC50 = 1500.0 nM 5.82
CHEMBL378963 IC50 = 3000.0 nM 5.52
CHEMBL210246 IC50 - -
CHEMBL207544 IC50 - -