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Assay Detail

CHEMBL997786

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

Binding
Inhibition of CDK2
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies.
Patel DS, Bharatam PV.
Eur J Med Chem (2008) 43 : 949 -957
PubMed 17707953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.23 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260416 1 8.70
CHEMBL500804 1 8.30
CHEMBL427909 1 8.30
CHEMBL260417 1 8.30
CHEMBL407981 1 7.22
CHEMBL318522 1 6.47
CHEMBL260928 1 6.32
CHEMBL260929 1 6.30
CHEMBL421207 1 6.20
CHEMBL260231 1 6.19
CHEMBL259270 1 -
CHEMBL317657 1 -
CHEMBL101747 1 -
CHEMBL406644 1 -
CHEMBL261690 1 -
CHEMBL408564 1 -
CHEMBL101804 1 -
CHEMBL407980 1 -
CHEMBL260243 1 -
CHEMBL261660 1 -
CHEMBL407113 1 -
CHEMBL261659 1 -
CHEMBL405021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260416 IC50 = 2.0 nM 8.70
CHEMBL500804 IC50 = 5.0 nM 8.30
CHEMBL427909 IC50 = 5.0 nM 8.30
CHEMBL260417 IC50 = 5.0 nM 8.30
CHEMBL407981 IC50 = 60.0 nM 7.22
CHEMBL318522 IC50 = 341.0 nM 6.47
CHEMBL260928 IC50 = 484.0 nM 6.32
CHEMBL260929 IC50 = 497.0 nM 6.30
CHEMBL421207 IC50 = 631.0 nM 6.20
CHEMBL260231 IC50 = 639.0 nM 6.19
CHEMBL259270 IC50 > 1000.0 nM -
CHEMBL317657 IC50 > 1000.0 nM -
CHEMBL101747 IC50 > 1000.0 nM -
CHEMBL406644 IC50 > 1000.0 nM -
CHEMBL261690 IC50 > 1000.0 nM -
CHEMBL408564 IC50 > 1000.0 nM -
CHEMBL101804 IC50 > 1000.0 nM -
CHEMBL407980 IC50 > 1000.0 nM -
CHEMBL260243 IC50 > 1000.0 nM -
CHEMBL261660 IC50 > 1000.0 nM -
CHEMBL407113 IC50 > 1000.0 nM -
CHEMBL261659 IC50 > 1000.0 nM -
CHEMBL405021 IC50 > 1000.0 nM -