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Assay Detail

CHEMBL4392763

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

Binding
Inhibition of recombinant human GSK3beta using prephosphorylated peptide as substrate measured after 30 mins by Kinase-glo luminescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-Aryl-3-(4-methoxybenzyl)ureas as potentially irreversible glycogen synthase kinase 3 inhibitors: Synthesis and biological evaluation.
Venter J, Perez C, van Otterlo WAL, Martínez A, Blackie MAL.
Bioorg Med Chem Lett (2019) 29 : 1597 -1600
PubMed 31054862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.23 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259850 1 7.14
CHEMBL4447545 1 7.07
CHEMBL1824333 1 6.96
CHEMBL4546384 1 6.89
CHEMBL4452731 1 6.58
CHEMBL4532931 1 6.11
CHEMBL4516941 1 5.74
CHEMBL4452831 1 5.65
CHEMBL4556827 1 5.61
CHEMBL4573681 1 5.39
CHEMBL4571262 1 5.38
CHEMBL4437756 1 -
CHEMBL4461606 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259850 IC50 = 72.0 nM 7.14
CHEMBL4447545 IC50 = 86.0 nM 7.07
CHEMBL1824333 IC50 = 110.0 nM 6.96
CHEMBL4546384 IC50 = 130.0 nM 6.89
CHEMBL4452731 IC50 = 260.0 nM 6.58
CHEMBL4532931 IC50 = 770.0 nM 6.11
CHEMBL4516941 IC50 = 1820.0 nM 5.74
CHEMBL4452831 IC50 = 2260.0 nM 5.65
CHEMBL4556827 IC50 = 2470.0 nM 5.61
CHEMBL4573681 IC50 = 4050.0 nM 5.39
CHEMBL4571262 IC50 = 4210.0 nM 5.38
CHEMBL4437756 IC50 > 10000.0 nM -
CHEMBL4461606 IC50 > 10000.0 nM -