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Assay Detail

CHEMBL1103280

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

Binding
Inhibition of human recombinant CDK2/cyclin A expressed in baculovirus-infected insect Sf21 cells after 10 mins
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.
Ibrahim DA, El-Metwally AM.
Eur J Med Chem (2010) 45 : 1158 -1166
PubMed 20045222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.16 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1077085 1 6.52
CHEMBL1077107 1 6.40
CHEMBL1087791 RESCOVITINE 1 6.30
CHEMBL1083509 1 6.05
CHEMBL1077070 1 6.05
CHEMBL1087566 1 5.51
CHEMBL1083817 1 5.42
CHEMBL280074 OLOMOUCINE 1 5.16
CHEMBL1086151 1 5.09
CHEMBL1087440 1 4.99
CHEMBL1077069 1 4.94
CHEMBL1082230 1 4.64
CHEMBL1087055 1 4.61
CHEMBL1087054 1 4.59
CHEMBL1077086 1 4.55
CHEMBL1084117 1 4.35
CHEMBL1084118 1 4.33
CHEMBL1086152 1 4.32
CHEMBL1077068 1 4.24
CHEMBL1077095 1 -
CHEMBL1088348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1077085 IC50 = 300.0 nM 6.52
CHEMBL1077107 IC50 = 400.0 nM 6.40
CHEMBL1087791 RESCOVITINE IC50 = 500.0 nM 6.30
CHEMBL1083509 IC50 = 900.0 nM 6.05
CHEMBL1077070 IC50 = 900.0 nM 6.05
CHEMBL1087566 IC50 = 3100.0 nM 5.51
CHEMBL1083817 IC50 = 3800.0 nM 5.42
CHEMBL280074 OLOMOUCINE IC50 = 7000.0 nM 5.16
CHEMBL1086151 IC50 = 8100.0 nM 5.09
CHEMBL1087440 IC50 = 10300.0 nM 4.99
CHEMBL1077069 IC50 = 11500.0 nM 4.94
CHEMBL1082230 IC50 = 22900.0 nM 4.64
CHEMBL1087055 IC50 = 24600.0 nM 4.61
CHEMBL1087054 IC50 = 25400.0 nM 4.59
CHEMBL1077086 IC50 = 28200.0 nM 4.55
CHEMBL1084117 IC50 = 44900.0 nM 4.35
CHEMBL1084118 IC50 = 46800.0 nM 4.33
CHEMBL1086152 IC50 = 48300.0 nM 4.32
CHEMBL1077068 IC50 = 57500.0 nM 4.24
CHEMBL1077095 IC50 > 100000.0 nM -
CHEMBL1088348 IC50 > 100000.0 nM -