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Assay Detail

CHEMBL4004958

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

Binding
Inhibition of human GST-tagged CDK2/bovine His-tagged Cyclin A
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

CDK2/Bovine cyclin A (CHEMBL4106153)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.
Coxon CR, Anscombe E, Harnor SJ, Martin MP, Carbain B, Golding BT, Hardcastle IR, Harlow LK, Korolchuk S, Matheson CJ, Newell DR, Noble ME, Sivaprakasam M, Tudhope SJ, Turner DM, Wang LZ, Wedge SR, Wong C, Griffin RJ, Endicott JA, Cano C.
J Med Chem (2017) 60 : 1746 -1767
PubMed 28005359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.66 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103249 1 9.00
CHEMBL4092981 1 8.70
CHEMBL4078988 1 8.52
CHEMBL4102518 1 8.10
CHEMBL4078246 1 8.00
CHEMBL4065402 1 7.77
CHEMBL4085238 1 7.75
CHEMBL4086832 1 7.72
CHEMBL4069161 1 7.72
CHEMBL4105278 1 7.62
CHEMBL4062554 1 7.58
CHEMBL4101626 1 7.58
CHEMBL4081027 1 7.41
CHEMBL4070391 1 7.36
CHEMBL4097571 1 7.28
CHEMBL4090226 1 6.66
CHEMBL4094205 1 6.54
CHEMBL4089837 1 6.24
CHEMBL4074015 1 6.08
CHEMBL122264 1 6.01
CHEMBL4061761 1 5.85
CHEMBL4073211 1 5.82
CHEMBL4102300 1 5.19
CHEMBL4081980 1 5.17
CHEMBL4084337 1 5.05
CHEMBL4072216 1 4.80
CHEMBL4066675 1 4.75
CHEMBL4094562 1 4.68
CHEMBL4099986 1 4.55
CHEMBL4072170 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103249 IC50 = 1.0 nM 9.00
CHEMBL4092981 IC50 = 2.0 nM 8.70
CHEMBL4078988 IC50 = 3.0 nM 8.52
CHEMBL4102518 IC50 = 8.0 nM 8.10
CHEMBL4078246 IC50 = 10.0 nM 8.00
CHEMBL4065402 IC50 = 17.0 nM 7.77
CHEMBL4085238 IC50 = 18.0 nM 7.75
CHEMBL4086832 IC50 = 19.0 nM 7.72
CHEMBL4069161 IC50 = 19.0 nM 7.72
CHEMBL4105278 IC50 = 24.0 nM 7.62
CHEMBL4062554 IC50 = 26.0 nM 7.58
CHEMBL4101626 IC50 = 26.0 nM 7.58
CHEMBL4081027 IC50 = 39.0 nM 7.41
CHEMBL4070391 IC50 = 44.0 nM 7.36
CHEMBL4097571 IC50 = 52.0 nM 7.28
CHEMBL4090226 IC50 = 220.0 nM 6.66
CHEMBL4094205 IC50 = 290.0 nM 6.54
CHEMBL4089837 IC50 = 580.0 nM 6.24
CHEMBL4074015 IC50 = 830.0 nM 6.08
CHEMBL122264 IC50 = 970.0 nM 6.01
CHEMBL4061761 IC50 = 1400.0 nM 5.85
CHEMBL4073211 IC50 = 1500.0 nM 5.82
CHEMBL4102300 IC50 = 6400.0 nM 5.19
CHEMBL4081980 IC50 = 6700.0 nM 5.17
CHEMBL4084337 IC50 = 8900.0 nM 5.05
CHEMBL4072216 IC50 = 16000.0 nM 4.80
CHEMBL4066675 IC50 = 18000.0 nM 4.75
CHEMBL4094562 IC50 = 21000.0 nM 4.68
CHEMBL4099986 IC50 = 28400.0 nM 4.55
CHEMBL4072170 IC50 = 61000.0 nM 4.21