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Assay Detail

CHEMBL4004948

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Binding
Inhibition of CDK2 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
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 5 6.62 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088242 1 9.10
CHEMBL319467 1 8.30
CHEMBL269881 1 4.77
CHEMBL259244 1 4.31
CHEMBL226395 METHYLGUANINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088242 IC50 = 0.8 nM 9.10
CHEMBL319467 IC50 = 5.0 nM 8.30
CHEMBL269881 IC50 = 17000.0 nM 4.77
CHEMBL259244 IC50 = 49000.0 nM 4.31
CHEMBL226395 METHYLGUANINE IC50 > 100000.0 nM -