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Assay Detail

CHEMBL2390763

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

Binding
Inhibition of human GSK3beta-mediated YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE phosphorylation
31
Total Activities
31
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

Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis.
Gunosewoyo H, Midzak A, Gaisina IN, Sabath EV, Fedolak A, Hanania T, Brunner D, Papadopoulos V, Kozikowski AP.
J Med Chem (2013) 56 : 5115 -5129
PubMed 23725591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.91 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386094 1 10.89
CHEMBL2386090 1 9.70
CHEMBL2386093 1 9.28
CHEMBL2386091 1 9.23
CHEMBL2386272 1 9.06
CHEMBL2386092 1 8.72
CHEMBL2386088 1 8.43
CHEMBL368248 1 8.38
CHEMBL2386096 1 8.32
CHEMBL2386112 1 8.28
CHEMBL2386106 1 8.28
CHEMBL2386273 1 7.95
CHEMBL2386089 1 7.94
CHEMBL2386097 1 7.82
CHEMBL2386108 1 7.75
CHEMBL2386102 1 7.70
CHEMBL489422 1 7.68
CHEMBL2386095 1 7.67
CHEMBL2386107 1 7.60
CHEMBL2386105 1 7.45
CHEMBL2386103 1 7.40
CHEMBL2386099 1 7.39
CHEMBL2386109 1 7.24
CHEMBL2386110 1 7.18
CHEMBL2386104 1 7.08
CHEMBL2386098 1 6.94
CHEMBL2386275 1 6.94
CHEMBL2386111 1 6.90
CHEMBL2386274 1 6.83
CHEMBL2386101 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386094 IC50 = 0.013 nM 10.89
CHEMBL2386090 IC50 = 0.2 nM 9.70
CHEMBL2386093 IC50 = 0.53 nM 9.28
CHEMBL2386091 IC50 = 0.59 nM 9.23
CHEMBL2386272 IC50 = 0.87 nM 9.06
CHEMBL2386092 IC50 = 1.9 nM 8.72
CHEMBL2386088 IC50 = 3.7 nM 8.43
CHEMBL368248 IC50 = 4.2 nM 8.38
CHEMBL2386096 IC50 = 4.8 nM 8.32
CHEMBL2386112 IC50 = 5.3 nM 8.28
CHEMBL2386106 IC50 = 5.3 nM 8.28
CHEMBL2386273 IC50 = 11.2 nM 7.95
CHEMBL2386089 IC50 = 11.5 nM 7.94
CHEMBL2386097 IC50 = 15.0 nM 7.82
CHEMBL2386108 IC50 = 17.6 nM 7.75
CHEMBL2386102 IC50 = 19.8 nM 7.70
CHEMBL489422 IC50 = 21.1 nM 7.68
CHEMBL2386095 IC50 = 21.4 nM 7.67
CHEMBL2386107 IC50 = 25.2 nM 7.60
CHEMBL2386105 IC50 = 35.7 nM 7.45
CHEMBL2386103 IC50 = 39.7 nM 7.40
CHEMBL2386099 IC50 = 41.1 nM 7.39
CHEMBL2386109 IC50 = 58.2 nM 7.24
CHEMBL2386110 IC50 = 65.9 nM 7.18
CHEMBL2386104 IC50 = 82.3 nM 7.08
CHEMBL2386098 IC50 = 116.0 nM 6.94
CHEMBL2386275 IC50 = 114.0 nM 6.94
CHEMBL2386111 IC50 = 127.0 nM 6.90
CHEMBL2386274 IC50 = 148.0 nM 6.83
CHEMBL2386101 IC50 = 202.0 nM 6.70
CHEMBL2386100 IC50 = 404.0 nM 6.39