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Assay Detail

CHEMBL3856506

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

Binding
Inhibition of human recombinant CDK9/cyclin T expressed in baculovirus infected Sf9 insect cells using pRB (773 to 928 residues) as substrate after 30 mins by [gamma-33P]ATP based scintillation counting analysis
5
Total Activities
5
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 5 7.94 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270687 MERIOLIN 5 1 8.22
CHEMBL270686 MERIOLIN 3 1 8.22
CHEMBL270897 MERIOLIN 2 1 7.75
CHEMBL405665 MERIOLIN 1 1 7.58
CHEMBL270346 MERIOLIN 9 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270687 MERIOLIN 5 IC50 = 6.0 nM 8.22
CHEMBL270686 MERIOLIN 3 IC50 = 6.0 nM 8.22
CHEMBL270897 MERIOLIN 2 IC50 = 18.0 nM 7.75
CHEMBL405665 MERIOLIN 1 IC50 = 26.0 nM 7.58
CHEMBL270346 MERIOLIN 9 IC50 > 10000.0 nM -