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Assay Detail

CHEMBL5123370

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

Binding
Inhibition of CDK9/Cyclin T (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

CDK9/cyclin T1 (CHEMBL2111389)
Type PROTEIN COMPLEX
Organism Homo sapiens

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 6 8.24 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756595 ENITOCICLIB 1.0 1 8.52
CHEMBL4754493 BTX-A51 1.0 1 8.40
CHEMBL296468 BMS-387032 1.0 1 8.40
CHEMBL2103840 DINACICLIB 3.0 1 8.40
CHEMBL445813 AT-7519 2.0 1 8.00
CHEMBL428690 ALVOCIDIB 3.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756595 ENITOCICLIB IC50 = 3.0 nM 8.52
CHEMBL4754493 BTX-A51 IC50 = 4.0 nM 8.40
CHEMBL296468 BMS-387032 IC50 = 4.0 nM 8.40
CHEMBL2103840 DINACICLIB IC50 = 4.0 nM 8.40
CHEMBL445813 AT-7519 IC50 = 10.0 nM 8.00
CHEMBL428690 ALVOCIDIB IC50 = 20.0 nM 7.70