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Assay Detail

CHEMBL963374

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

Binding
Inhibition of human GSK3-beta by scintillation counting
40
Total Activities
40
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

From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
Gaisina IN, Gallier F, Ougolkov AV, Kim KH, Kurome T, Guo S, Holzle D, Luchini DN, Blond SY, Billadeau DD, Kozikowski AP.
J Med Chem (2009) 52 : 1853 -1863
PubMed 19338355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 7.40 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491647 1 9.64
CHEMBL477038 1 9.46
CHEMBL489833 1 9.29
CHEMBL490636 1 9.14
CHEMBL522590 1 9.02
CHEMBL490842 1 8.92
CHEMBL489210 1 8.46
CHEMBL491447 1 8.29
CHEMBL522464 1 8.27
CHEMBL489422 1 8.15
CHEMBL505673 1 8.12
CHEMBL490637 1 7.99
CHEMBL490861 1 7.88
CHEMBL503469 1 7.82
CHEMBL484685 1 7.79
CHEMBL516261 1 7.62
CHEMBL489435 1 7.60
CHEMBL522751 1 7.46
CHEMBL301138 1 7.46
CHEMBL523113 1 7.38
CHEMBL259850 1 7.38
CHEMBL489845 1 7.32
CHEMBL102714 SB-216763 1 7.30
CHEMBL489410 1 7.26
CHEMBL489043 1 7.05
CHEMBL490860 1 6.75
CHEMBL489407 1 6.74
CHEMBL520147 1 6.65
CHEMBL491064 1 6.63
CHEMBL523435 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491647 IC50 = 0.23 nM 9.64
CHEMBL477038 IC50 = 0.35 nM 9.46
CHEMBL489833 IC50 = 0.51 nM 9.29
CHEMBL490636 IC50 = 0.73 nM 9.14
CHEMBL522590 IC50 = 0.95 nM 9.02
CHEMBL490842 IC50 = 1.2 nM 8.92
CHEMBL489210 IC50 = 3.5 nM 8.46
CHEMBL491447 IC50 = 5.1 nM 8.29
CHEMBL522464 IC50 = 5.4 nM 8.27
CHEMBL489422 IC50 = 7.0 nM 8.15
CHEMBL505673 IC50 = 7.5 nM 8.12
CHEMBL490637 IC50 = 10.2 nM 7.99
CHEMBL490861 IC50 = 13.2 nM 7.88
CHEMBL503469 IC50 = 15.0 nM 7.82
CHEMBL484685 IC50 = 16.1 nM 7.79
CHEMBL516261 IC50 = 23.8 nM 7.62
CHEMBL489435 IC50 = 25.3 nM 7.60
CHEMBL522751 IC50 = 34.5 nM 7.46
CHEMBL301138 IC50 = 35.0 nM 7.46
CHEMBL259850 IC50 = 41.8 nM 7.38
CHEMBL523113 IC50 = 42.0 nM 7.38
CHEMBL489845 IC50 = 48.3 nM 7.32
CHEMBL102714 SB-216763 IC50 = 50.0 nM 7.30
CHEMBL489410 IC50 = 55.0 nM 7.26
CHEMBL489043 IC50 = 88.7 nM 7.05
CHEMBL490860 IC50 = 180.0 nM 6.75
CHEMBL489407 IC50 = 184.0 nM 6.74
CHEMBL520147 IC50 = 223.0 nM 6.65
CHEMBL491064 IC50 = 235.0 nM 6.63
CHEMBL523435 IC50 = 247.0 nM 6.61
CHEMBL522760 IC50 = 260.0 nM 6.58
CHEMBL491859 IC50 = 314.0 nM 6.50
CHEMBL490044 IC50 = 335.0 nM 6.47
CHEMBL483669 IC50 = 440.0 nM 6.36
CHEMBL483465 ELRAGLUSIB IC50 = 710.0 nM 6.15
CHEMBL482632 IC50 = 830.0 nM 6.08
CHEMBL521774 IC50 = 870.0 nM 6.06
CHEMBL490639 IC50 = 1290.0 nM 5.89
CHEMBL489413 IC50 = 4090.0 nM 5.39
CHEMBL489421 IC50 = 7160.0 nM 5.14