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Assay Detail

CHEMBL963375

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Binding
Inhibition of CDK2/Cyclin E
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2 (CHEMBL301)
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 14 6.02 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.42
CHEMBL491447 1 7.57
CHEMBL522464 1 6.83
CHEMBL477038 1 6.62
CHEMBL489833 1 6.47
CHEMBL522751 1 5.97
CHEMBL505673 1 5.94
CHEMBL301138 1 5.85
CHEMBL523113 1 5.74
CHEMBL491647 1 5.41
CHEMBL522590 1 4.93
CHEMBL491064 1 4.50
CHEMBL522760 1 4.00
CHEMBL523435 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 3.8 nM 8.42
CHEMBL491447 IC50 = 27.0 nM 7.57
CHEMBL522464 IC50 = 149.0 nM 6.83
CHEMBL477038 IC50 = 237.0 nM 6.62
CHEMBL489833 IC50 = 337.0 nM 6.47
CHEMBL522751 IC50 = 1070.0 nM 5.97
CHEMBL505673 IC50 = 1160.0 nM 5.94
CHEMBL301138 IC50 = 1410.0 nM 5.85
CHEMBL523113 IC50 = 1840.0 nM 5.74
CHEMBL491647 IC50 = 3880.0 nM 5.41
CHEMBL522590 IC50 = 11700.0 nM 4.93
CHEMBL491064 IC50 = 32000.0 nM 4.50
CHEMBL522760 IC50 = 99000.0 nM 4.00
CHEMBL523435 IC50 > 50000.0 nM -