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Assay Detail

CHEMBL4386151

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

Binding
Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-33P]ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK9/cyclin T1 (CHEMBL2111389)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Jorda R, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T, Široká J, Urbánek L, Pachl P, Řezáčová P, Strnad M, Klener P, Kryštof V.
J Med Chem (2019) 62 : 4606 -4623
PubMed 30943029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.33 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 7.82
CHEMBL4540226 1 7.60
CHEMBL518800 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 15.0 nM 7.82
CHEMBL4540226 IC50 = 25.0 nM 7.60
CHEMBL518800 IC50 = 272.0 nM 6.57