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Assay Detail

CHEMBL2215732

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Binding
Inhibition of GSK3beta by kinase-glo assay method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glycogen synthase kinase-3 beta (CHEMBL262)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.
Zhang P, Hu HR, Huang ZH, Lei JY, Chu Y, Ye DY.
Bioorg Med Chem Lett (2012) 22 : 7232 -7236
PubMed 23099099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.69 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284861 1 5.85
CHEMBL2207940 1 4.60
CHEMBL2207939 1 4.57
CHEMBL2207946 1 4.32
CHEMBL2207938 1 4.11
CHEMBL2207947 1 -
CHEMBL1492321 1 -
CHEMBL2207945 1 -
CHEMBL2207944 1 -
CHEMBL2207943 1 -
CHEMBL2207942 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284861 IC50 = 1400.0 nM 5.85
CHEMBL2207940 IC50 = 25000.0 nM 4.60
CHEMBL2207939 IC50 = 27000.0 nM 4.57
CHEMBL2207946 IC50 = 47500.0 nM 4.32
CHEMBL2207938 IC50 = 77200.0 nM 4.11
CHEMBL2207947 IC50 > 100000.0 nM -
CHEMBL1492321 IC50 > 100000.0 nM -
CHEMBL2207945 IC50 > 100000.0 nM -
CHEMBL2207944 IC50 > 100000.0 nM -
CHEMBL2207943 IC50 = 480000.0 nM -
CHEMBL2207942 IC50 = 830000.0 nM -