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Assay Detail

CHEMBL4386147

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

Binding
Inhibition of GST-tagged CDK2/Cyclin-A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate measured in presence of [gamma-33P]ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

CDK2/Cyclin A2 (CHEMBL3038469)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Jorda R, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T, Široká J, Urbánek L, Pachl P, Řezáčová P, Strnad M, Klener P, Kryštof V.
J Med Chem (2019) 62 : 4606 -4623
PubMed 30943029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.86 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 8.52
CHEMBL4540226 1 8.22
CHEMBL518800 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 3.0 nM 8.52
CHEMBL4540226 IC50 = 6.0 nM 8.22
CHEMBL518800 IC50 = 144.0 nM 6.84