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Assay Detail

CHEMBL5136672

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

Binding
Inhibition of GST-tagged CDK2/cyclin D1 (unknown origin) expressed in Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay
7
Total Activities
7
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

Cyclin-dependent kinase 2/G1/S-specific cyclin-D1 (CHEMBL3885552)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3,5,7-Substituted Pyrazolo[4,3-<i>d</i>]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders.
Jorda R, Havlíček L, Peřina M, Vojáčková V, Pospíšil T, Djukic S, Škerlová J, Grúz J, Renešová N, Klener P, Řezáčová P, Strnad M, Kryštof V.
J Med Chem (2022) 65 : 8881 -8896
PubMed 35749742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.49 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 6.94
CHEMBL5169449 1 6.03
CHEMBL5191136 1 -
CHEMBL5182767 1 -
CHEMBL5187378 1 -
CHEMBL5194202 1 -
CHEMBL5194833 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 115.0 nM 6.94
CHEMBL5169449 IC50 = 940.0 nM 6.03
CHEMBL5191136 IC50 > 1000.0 nM -
CHEMBL5182767 IC50 > 1000.0 nM -
CHEMBL5187378 IC50 > 1000.0 nM -
CHEMBL5194202 IC50 > 1000.0 nM -
CHEMBL5194833 IC50 > 1000.0 nM -