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Assay Detail

CHEMBL3856474

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

Binding
Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 3 8.22 8.40
Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296468 BMS-387032 1.0 1 8.40
CHEMBL4442620 RONICICLIB 2.0 1 8.30
CHEMBL428690 ALVOCIDIB 3.0 1 7.96
CHEMBL445813 AT-7519 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296468 BMS-387032 IC50 = 4.0 nM 8.40
CHEMBL4442620 RONICICLIB IC50 = 5.0 nM 8.30
CHEMBL428690 ALVOCIDIB IC50 = 11.0 nM 7.96
CHEMBL445813 AT-7519 Ki < 100.0 nM -