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Assay Detail

CHEMBL4679477

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

Binding
Inhibition of human full-length N-terminal GST-fused CDK9 (1 to 372 residues)/His-tagged Cyclin-T1 (1 to 726 residues) expressed in baculovirus expression system using PEP as substrate incubated for 17 mins in presence of ATP by TR-FRET assay
12
Total Activities
12
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

Cyclin-Dependent Kinase Inhibitors in Cancer Therapeutics.
Kargbo RB
ACS Med Chem Lett (2021) 12 : 11 -12
PubMed 33488958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.67 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3958430 1 8.22
CHEMBL4743130 1 8.21
CHEMBL4787666 1 8.15
CHEMBL4742853 1 8.15
CHEMBL4797439 1 8.12
CHEMBL4785428 1 7.63
CHEMBL4796706 1 7.50
CHEMBL4776293 1 7.33
CHEMBL4796549 1 7.15
CHEMBL4742131 1 7.09
CHEMBL4759094 1 6.83
CHEMBL4745518 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3958430 IC50 = 6.03 nM 8.22
CHEMBL4743130 IC50 = 6.18 nM 8.21
CHEMBL4787666 IC50 = 7.13 nM 8.15
CHEMBL4742853 IC50 = 7.08 nM 8.15
CHEMBL4797439 IC50 = 7.55 nM 8.12
CHEMBL4785428 IC50 = 23.4 nM 7.63
CHEMBL4796706 IC50 = 31.8 nM 7.50
CHEMBL4776293 IC50 = 46.6 nM 7.33
CHEMBL4796549 IC50 = 70.7 nM 7.15
CHEMBL4742131 IC50 = 80.5 nM 7.09
CHEMBL4759094 IC50 = 149.0 nM 6.83
CHEMBL4745518 IC50 < 3.2 nM -