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Assay Detail

CHEMBL2406225

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

Binding
Inhibition of human recombinant CDK2/Cyclin E expressed in baculovirus infected sf9 cells using histone H1 as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.
Gucký T, Jorda R, Zatloukal M, Bazgier V, Berka K, Řezníčková E, Béres T, Strnad M, Kryštof V.
J Med Chem (2013) 56 : 6234 -6247
PubMed 23829517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.63 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2403096 1 8.40
CHEMBL2402946 1 8.15
CHEMBL2402947 1 8.10
CHEMBL2403095 1 8.10
CHEMBL2403094 1 8.00
CHEMBL2403091 1 8.00
CHEMBL2403084 1 7.94
CHEMBL2403088 1 7.92
CHEMBL2403085 1 7.89
CHEMBL2403093 1 7.85
CHEMBL2403087 1 7.85
CHEMBL2403097 1 7.75
CHEMBL2402948 1 7.75
CHEMBL2403086 1 7.70
CHEMBL2402953 1 7.69
CHEMBL2403098 1 7.64
CHEMBL2402952 1 7.58
CHEMBL2403090 1 7.51
CHEMBL2402954 1 7.48
CHEMBL2403092 1 7.47
CHEMBL2403083 1 7.47
CHEMBL2402949 1 7.39
CHEMBL150261 1 7.32
CHEMBL2402945 1 7.17
CHEMBL2403099 1 6.92
CHEMBL14762 SELICICLIB 2.0 1 6.77
CHEMBL2403089 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2403096 IC50 = 4.0 nM 8.40
CHEMBL2402946 IC50 = 7.1 nM 8.15
CHEMBL2402947 IC50 = 8.0 nM 8.10
CHEMBL2403095 IC50 = 8.0 nM 8.10
CHEMBL2403094 IC50 = 10.0 nM 8.00
CHEMBL2403091 IC50 = 10.0 nM 8.00
CHEMBL2403084 IC50 = 11.4 nM 7.94
CHEMBL2403088 IC50 = 12.0 nM 7.92
CHEMBL2403085 IC50 = 13.0 nM 7.89
CHEMBL2403093 IC50 = 14.0 nM 7.85
CHEMBL2403087 IC50 = 14.0 nM 7.85
CHEMBL2403097 IC50 = 18.0 nM 7.75
CHEMBL2402948 IC50 = 18.0 nM 7.75
CHEMBL2403086 IC50 = 20.0 nM 7.70
CHEMBL2402953 IC50 = 20.5 nM 7.69
CHEMBL2403098 IC50 = 23.0 nM 7.64
CHEMBL2402952 IC50 = 26.0 nM 7.58
CHEMBL2403090 IC50 = 31.0 nM 7.51
CHEMBL2402954 IC50 = 33.0 nM 7.48
CHEMBL2403092 IC50 = 34.0 nM 7.47
CHEMBL2403083 IC50 = 33.5 nM 7.47
CHEMBL2402949 IC50 = 40.7 nM 7.39
CHEMBL150261 IC50 = 48.0 nM 7.32
CHEMBL2402945 IC50 = 68.0 nM 7.17
CHEMBL2403099 IC50 = 120.0 nM 6.92
CHEMBL14762 SELICICLIB IC50 = 170.0 nM 6.77
CHEMBL2403089 IC50 = 478.0 nM 6.32