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Assay Detail

CHEMBL1685181

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

Binding
Inhibition of human recombinant GSK3-beta expressed in baculovirus infected SF9 cells after 60 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors.
Coffman K, Brodney M, Cook J, Lanyon L, Pandit J, Sakya S, Schachter J, Tseng-Lovering E, Wessel M.
Bioorg Med Chem Lett (2011) 21 : 1429 -1433
PubMed 21295469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.36 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1682851 1 8.21
CHEMBL1682850 1 8.07
CHEMBL1682842 1 7.76
CHEMBL501724 1 7.76
CHEMBL1682838 1 7.30
CHEMBL1682849 1 7.29
CHEMBL1682839 1 7.21
CHEMBL1682852 1 7.20
CHEMBL1682848 1 7.08
CHEMBL1682853 1 6.94
CHEMBL1682847 1 6.88
CHEMBL1682840 1 6.63
CHEMBL1682845 1 -
CHEMBL1682846 1 -
CHEMBL1682844 1 -
CHEMBL1682843 1 -
CHEMBL1682841 1 -
CHEMBL1682837 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1682851 IC50 = 6.1 nM 8.21
CHEMBL1682850 IC50 = 8.5 nM 8.07
CHEMBL1682842 IC50 = 17.4 nM 7.76
CHEMBL501724 IC50 = 17.2 nM 7.76
CHEMBL1682838 IC50 = 50.1 nM 7.30
CHEMBL1682849 IC50 = 51.0 nM 7.29
CHEMBL1682839 IC50 = 62.0 nM 7.21
CHEMBL1682852 IC50 = 62.8 nM 7.20
CHEMBL1682848 IC50 = 84.1 nM 7.08
CHEMBL1682853 IC50 = 115.0 nM 6.94
CHEMBL1682847 IC50 = 133.0 nM 6.88
CHEMBL1682840 IC50 = 233.0 nM 6.63
CHEMBL1682845 IC50 > 252.0 nM -
CHEMBL1682846 IC50 > 260.0 nM -
CHEMBL1682844 IC50 > 731.0 nM -
CHEMBL1682843 IC50 > 401.0 nM -
CHEMBL1682841 IC50 > 592.0 nM -
CHEMBL1682837 IC50 > 894.0 nM -