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Assay Detail

CHEMBL5098671

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

Binding
Inhibition of CDK9 (unknown origin) using FITC-X-GSRTPMY-NH2 as substrate preincubated for 10 mins followed by substrate addition and measured after 90 mins in the presence of ATP at Km concentration by plate reader analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 9 (CHEMBL3116)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Barlaam B, De Savi C, Dishington A, Drew L, Ferguson AD, Ferguson D, Gu C, Hande S, Hassall L, Hawkins J, Hird AW, Holmes J, Lamb ML, Lister AS, McGuire TM, Moore JE, O'Connell N, Patel A, Pike KG, Sarkar U, Shao W, Stead D, Varnes JG, Vasbinder MM, Wang L, Wu L, Xue L, Yang B, Yao T.
J Med Chem (2021) 64 : 15189 -15213
PubMed 34647738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.64 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5173041 1 8.05
CHEMBL5207813 1 8.00
CHEMBL5188442 1 7.72
CHEMBL5201044 1 7.47
CHEMBL5191333 1 7.33
CHEMBL5192139 1 7.24
CHEMBL5170195 1 -
CHEMBL3663760 1 -
CHEMBL5170524 1 -
CHEMBL5197170 1 -
CHEMBL5198038 1 -
CHEMBL5207871 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5173041 IC50 = 9.0 nM 8.05
CHEMBL5207813 IC50 = 10.0 nM 8.00
CHEMBL5188442 IC50 = 19.0 nM 7.72
CHEMBL5201044 IC50 = 34.0 nM 7.47
CHEMBL5191333 IC50 = 47.0 nM 7.33
CHEMBL5192139 IC50 = 57.0 nM 7.24
CHEMBL5170195 IC50 < 3.0 nM -
CHEMBL3663760 IC50 < 3.0 nM -
CHEMBL5170524 IC50 < 3.0 nM -
CHEMBL5197170 IC50 < 3.0 nM -
CHEMBL5198038 IC50 < 3.0 nM -
CHEMBL5207871 IC50 < 3.0 nM -