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Assay Detail

CHEMBL2013356

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

Binding
Inhibition of CDK2
21
Total Activities
21
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

Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases.
Wang T, Block MA, Cowen S, Davies AM, Devereaux E, Gingipalli L, Johannes J, Larsen NA, Su Q, Tucker JA, Whitston D, Wu J, Zhang HJ, Zinda M, Chuaqui C.
Bioorg Med Chem Lett (2012) 22 : 2063 -2069
PubMed 22305584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.11 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011932 1 7.16
CHEMBL2011927 1 6.88
CHEMBL2011926 1 6.87
CHEMBL2011940 1 6.81
CHEMBL2011934 1 6.73
CHEMBL2011935 1 6.46
CHEMBL2011928 1 6.43
CHEMBL2011941 1 6.29
CHEMBL2011931 1 5.86
CHEMBL2010815 1 5.70
CHEMBL2011936 1 5.55
CHEMBL2011937 1 5.40
CHEMBL2011944 1 5.33
CHEMBL2011945 1 5.19
CHEMBL2011942 1 5.03
CHEMBL2011938 1 -
CHEMBL2011939 1 -
CHEMBL2011933 1 -
CHEMBL2011930 1 -
CHEMBL2011943 1 -
CHEMBL2011929 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011932 IC50 = 70.0 nM 7.16
CHEMBL2011927 IC50 = 133.0 nM 6.88
CHEMBL2011926 IC50 = 135.0 nM 6.87
CHEMBL2011940 IC50 = 155.0 nM 6.81
CHEMBL2011934 IC50 = 187.0 nM 6.73
CHEMBL2011935 IC50 = 345.0 nM 6.46
CHEMBL2011928 IC50 = 370.0 nM 6.43
CHEMBL2011941 IC50 = 518.0 nM 6.29
CHEMBL2011931 IC50 = 1370.0 nM 5.86
CHEMBL2010815 IC50 = 2020.0 nM 5.70
CHEMBL2011936 IC50 = 2790.0 nM 5.55
CHEMBL2011937 IC50 = 3970.0 nM 5.40
CHEMBL2011944 IC50 = 4650.0 nM 5.33
CHEMBL2011945 IC50 = 6520.0 nM 5.19
CHEMBL2011942 IC50 = 9410.0 nM 5.03
CHEMBL2011938 IC50 - -
CHEMBL2011939 IC50 - -
CHEMBL2011933 IC50 > 4910.0 nM -
CHEMBL2011930 IC50 > 30000.0 nM -
CHEMBL2011943 IC50 > 30000.0 nM -
CHEMBL2011929 IC50 > 5280.0 nM -