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Assay Detail

CHEMBL4048312

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

Binding
Inhibition of CDK9/cyclin T1 (unknown origin) using YSPTSPSYSPTSPSYSPTSPKKK as substrate after 30 mins in presence of [33P]-gamma-ATP by filter binding assay
10
Total Activities
10
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

Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.
Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M, Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA.
J Med Chem (2018) 61 : 1664 -1687
PubMed 29370702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.08 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079206 1 8.72
CHEMBL4103469 1 7.94
CHEMBL4066369 1 7.54
CHEMBL4100359 1 7.18
CHEMBL4074270 1 6.80
CHEMBL4094775 1 6.58
CHEMBL4065874 1 6.55
CHEMBL1077604 ROHITUKINE 1 6.52
CHEMBL4105395 1 6.51
CHEMBL4087077 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079206 IC50 = 1.9 nM 8.72
CHEMBL4103469 IC50 = 11.5 nM 7.94
CHEMBL4066369 IC50 = 29.0 nM 7.54
CHEMBL4100359 IC50 = 66.0 nM 7.18
CHEMBL4074270 IC50 = 160.0 nM 6.80
CHEMBL4094775 IC50 = 260.0 nM 6.58
CHEMBL4065874 IC50 = 280.0 nM 6.55
CHEMBL1077604 ROHITUKINE IC50 = 300.0 nM 6.52
CHEMBL4105395 IC50 = 310.0 nM 6.51
CHEMBL4087077 IC50 = 350.0 nM 6.46