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Assay Detail

CHEMBL3807243

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

Binding
Inhibition of full length human recombinant His-tagged CDK9/Cyclin T expressed in baculovirus expression system using Cdk7/9tide as substrate by adapta assay
2
Total Activities
2
Compounds Tested
1
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

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.
Koehler MF, Bergeron P, Blackwood EM, Bowman K, Clark KR, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini MH.
ACS Med Chem Lett (2016) 7 : 223 -228
PubMed 26985305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.81 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3805194 1 5.96
CHEMBL118518 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3805194 IC50 = 1100.0 nM 5.96
CHEMBL118518 IC50 = 2200.0 nM 5.66