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Assay Detail

CHEMBL5123367

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

Binding
Inhibition of CDK2/Cyclin E (unknown origin)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.
Shi Z, Tian L, Qiang T, Li J, Xing Y, Ren X, Liu C, Liang C.
J Med Chem (2022) 65 : 6390 -6418
PubMed 35485642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.37 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51709 1 9.51
CHEMBL2103840 DINACICLIB 3.0 1 9.00
CHEMBL5196505 1 8.97
CHEMBL5201870 TEGTOCICLIB 2.0 1 8.94
CHEMBL4650328 AVOTACICLIB 1.0 1 8.82
CHEMBL5176598 1 8.68
CHEMBL5178317 1 8.68
CHEMBL384304 RG-547 2.0 1 8.52
CHEMBL4741442 1 8.40
CHEMBL4442620 RONICICLIB 2.0 1 8.05
CHEMBL216126 1 7.62
CHEMBL48362 1 7.52
CHEMBL296468 BMS-387032 1.0 1 7.42
CHEMBL428690 ALVOCIDIB 3.0 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51709 IC50 = 0.31 nM 9.51
CHEMBL2103840 DINACICLIB IC50 = 1.0 nM 9.00
CHEMBL5196505 IC50 = 1.07 nM 8.97
CHEMBL5201870 TEGTOCICLIB IC50 = 1.16 nM 8.94
CHEMBL4650328 AVOTACICLIB IC50 = 1.5 nM 8.82
CHEMBL5176598 IC50 = 2.11 nM 8.68
CHEMBL5178317 IC50 = 2.1 nM 8.68
CHEMBL384304 RG-547 IC50 = 3.0 nM 8.52
CHEMBL4741442 IC50 = 4.0 nM 8.40
CHEMBL4442620 RONICICLIB IC50 = 9.0 nM 8.05
CHEMBL216126 IC50 = 24.0 nM 7.62
CHEMBL48362 IC50 = 30.0 nM 7.52
CHEMBL296468 BMS-387032 IC50 = 38.0 nM 7.42
CHEMBL428690 ALVOCIDIB IC50 = 100.0 nM 7.00