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Assay Detail

CHEMBL3856498

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

Binding
Inhibition of human His6-tagged CDK9/cyclin T1 expressed in baculovirus infected sf9 cells using GST-CTD as substrate after 10 mins in presence of [gamma-32P]ATP by SDS-PAGE analysis
9
Total Activities
9
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

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

Publication

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
Sonawane YA, Taylor MA, Napoleon JV, Rana S, Contreras JI, Natarajan A.
J Med Chem (2016) 59 : 8667 -8684
PubMed 27171036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.23 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3896233 1 8.68
CHEMBL428690 ALVOCIDIB 3.0 1 8.60
CHEMBL3924246 1 8.55
CHEMBL3915260 1 8.26
CHEMBL3976972 1 8.19
CHEMBL3898028 1 8.05
CHEMBL3906282 1 8.02
CHEMBL3985045 1 8.02
CHEMBL3897316 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3896233 IC50 = 2.1 nM 8.68
CHEMBL428690 ALVOCIDIB IC50 = 2.5 nM 8.60
CHEMBL3924246 IC50 = 2.8 nM 8.55
CHEMBL3915260 IC50 = 5.5 nM 8.26
CHEMBL3976972 IC50 = 6.5 nM 8.19
CHEMBL3898028 IC50 = 9.0 nM 8.05
CHEMBL3906282 IC50 = 9.6 nM 8.02
CHEMBL3985045 IC50 = 9.5 nM 8.02
CHEMBL3897316 IC50 = 19.0 nM 7.72