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Assay Detail

CHEMBL4189175

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Binding
Inhibition of recombinant human CDK2/cyclin A using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by fluorescence assay relative to control
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel CDK inhibitors via scaffold hopping from CAN508.
Jing L, Tang Y, Xiao Z.
Bioorg Med Chem Lett (2018) 28 : 1386 -1391
PubMed 29550093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.86 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4208708 1 6.44
CHEMBL4211730 1 6.18
CHEMBL4214475 1 6.09
CHEMBL4216945 1 5.70
CHEMBL215205 1 4.88
CHEMBL4203594 1 -
CHEMBL4213114 1 -
CHEMBL4217525 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4208708 IC50 = 360.0 nM 6.44
CHEMBL4211730 IC50 = 660.0 nM 6.18
CHEMBL4214475 IC50 = 820.0 nM 6.09
CHEMBL4216945 IC50 = 2000.0 nM 5.70
CHEMBL215205 IC50 = 13100.0 nM 4.88
CHEMBL4203594 IC50 - -
CHEMBL4213114 IC50 - -
CHEMBL4217525 IC50 - -