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Assay Detail

CHEMBL5230717

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

Binding
Inhibition of CDK2 (unknown origin)
15
Total Activities
15
Compounds Tested
2
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

A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents.
Marak BN, Dowarah J, Khiangte L, Singh VP.
Eur J Med Chem (2020) 203 : 112571 -112571
PubMed 32707525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.90 9.00
Ki 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 9.00
CHEMBL384304 RG-547 2.0 1 8.52
CHEMBL488436 AZD-5438 1.0 1 8.22
CHEMBL1230607 PHA-793887 1.0 1 8.10
CHEMBL445813 AT-7519 2.0 1 8.00
CHEMBL428690 ALVOCIDIB 3.0 1 7.70
CHEMBL564829 MILCICLIB 2.0 1 7.35
CHEMBL5273925 1 7.32
CHEMBL5285495 1 6.80
CHEMBL5269468 1 6.52
CHEMBL14762 SELICICLIB 2.0 1 6.16
CHEMBL5280632 1 5.43
CHEMBL5275225 1 5.35
CHEMBL5280858 1 5.33
CHEMBL5281901 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 1.0 nM 9.00
CHEMBL384304 RG-547 Ki = 3.0 nM 8.52
CHEMBL488436 AZD-5438 IC50 = 6.0 nM 8.22
CHEMBL1230607 PHA-793887 IC50 = 8.0 nM 8.10
CHEMBL445813 AT-7519 IC50 = 10.0 nM 8.00
CHEMBL428690 ALVOCIDIB IC50 = 20.0 nM 7.70
CHEMBL564829 MILCICLIB IC50 = 45.0 nM 7.35
CHEMBL5273925 IC50 = 48.0 nM 7.32
CHEMBL5285495 IC50 = 160.0 nM 6.80
CHEMBL5269468 IC50 = 300.0 nM 6.52
CHEMBL14762 SELICICLIB IC50 = 700.0 nM 6.16
CHEMBL5280632 IC50 = 3700.0 nM 5.43
CHEMBL5275225 IC50 = 4500.0 nM 5.35
CHEMBL5280858 IC50 = 4630.0 nM 5.33
CHEMBL5281901 IC50 = 5200.0 nM 5.28