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Assay Detail

CHEMBL930273

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

Binding
Inhibition of recombinant GSK3-beta
151
Total Activities
151
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

Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.
Taha MO, Bustanji Y, Al-Ghussein MA, Mohammad M, Zalloum H, Al-Masri IM, Atallah N.
J Med Chem (2008) 51 : 2062 -2077
PubMed 18324764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 151 6.89 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260417 1 9.10
CHEMBL261129 1 9.00
CHEMBL260664 1 9.00
CHEMBL407981 1 8.40
CHEMBL258483 1 8.30
CHEMBL260416 1 8.30
CHEMBL259271 1 8.30
CHEMBL261518 1 8.30
CHEMBL260662 1 8.22
CHEMBL264161 1 8.15
CHEMBL408564 1 8.15
CHEMBL407980 1 8.15
CHEMBL259838 1 8.15
CHEMBL409738 1 8.15
CHEMBL261549 1 8.15
CHEMBL260345 1 8.10
CHEMBL405145 1 8.10
CHEMBL406125 1 8.05
CHEMBL407002 1 7.96
CHEMBL261441 1 7.96
CHEMBL410926 1 7.92
CHEMBL408019 1 7.92
CHEMBL317657 1 7.85
CHEMBL260163 1 7.82
CHEMBL406644 1 7.80
CHEMBL407373 1 7.75
CHEMBL260680 1 7.75
CHEMBL261596 1 7.72
CHEMBL263907 1 7.70
CHEMBL352222 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260417 IC50 = 0.8 nM 9.10
CHEMBL261129 IC50 = 1.0 nM 9.00
CHEMBL260664 IC50 = 1.0 nM 9.00
CHEMBL407981 IC50 = 4.0 nM 8.40
CHEMBL261518 IC50 = 5.0 nM 8.30
CHEMBL259271 IC50 = 5.0 nM 8.30
CHEMBL260416 IC50 = 5.0 nM 8.30
CHEMBL258483 IC50 = 5.0 nM 8.30
CHEMBL260662 IC50 = 6.0 nM 8.22
CHEMBL264161 IC50 = 7.0 nM 8.15
CHEMBL408564 IC50 = 7.0 nM 8.15
CHEMBL407980 IC50 = 7.0 nM 8.15
CHEMBL259838 IC50 = 7.0 nM 8.15
CHEMBL409738 IC50 = 7.0 nM 8.15
CHEMBL261549 IC50 = 7.0 nM 8.15
CHEMBL405145 IC50 = 8.0 nM 8.10
CHEMBL260345 IC50 = 8.0 nM 8.10
CHEMBL406125 IC50 = 9.0 nM 8.05
CHEMBL261441 IC50 = 11.0 nM 7.96
CHEMBL407002 IC50 = 11.0 nM 7.96
CHEMBL408019 IC50 = 12.0 nM 7.92
CHEMBL410926 IC50 = 12.0 nM 7.92
CHEMBL317657 IC50 = 14.0 nM 7.85
CHEMBL260163 IC50 = 15.0 nM 7.82
CHEMBL406644 IC50 = 16.0 nM 7.80
CHEMBL260680 IC50 = 18.0 nM 7.75
CHEMBL407373 IC50 = 18.0 nM 7.75
CHEMBL261596 IC50 = 19.0 nM 7.72
CHEMBL263907 IC50 = 20.0 nM 7.70
CHEMBL352222 IC50 = 20.0 nM 7.70
CHEMBL407730 IC50 = 21.0 nM 7.68
CHEMBL259744 IC50 = 22.0 nM 7.66
CHEMBL427909 IC50 = 24.0 nM 7.62
CHEMBL156379 IC50 = 26.0 nM 7.58
CHEMBL407003 IC50 = 27.0 nM 7.57
CHEMBL160586 IC50 = 28.0 nM 7.55
CHEMBL260243 IC50 = 35.0 nM 7.46
CHEMBL260663 IC50 = 36.0 nM 7.44
CHEMBL260231 IC50 = 39.0 nM 7.41
CHEMBL261659 IC50 = 42.0 nM 7.38
CHEMBL406701 IC50 = 43.0 nM 7.37
CHEMBL158885 IC50 = 52.0 nM 7.28
CHEMBL258701 IC50 = 56.0 nM 7.25
CHEMBL422714 IC50 = 58.0 nM 7.24
CHEMBL345348 IC50 = 59.0 nM 7.23
CHEMBL345801 IC50 = 70.0 nM 7.16
CHEMBL347681 IC50 = 71.0 nM 7.15
CHEMBL345212 IC50 = 74.0 nM 7.13
CHEMBL156987 IC50 = 76.0 nM 7.12
CHEMBL259270 IC50 = 75.0 nM 7.12