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Assay Detail

CHEMBL5136673

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

Binding
Inhibition of GST-tagged human CDK5/p25 expressed in Sf9 cells using histone H1 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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.23 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 7.89
CHEMBL5169449 1 7.62
CHEMBL5194202 1 7.41
CHEMBL5182767 1 7.27
CHEMBL5194833 1 6.90
CHEMBL5187378 1 6.80
CHEMBL5191136 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 13.0 nM 7.89
CHEMBL5169449 IC50 = 24.0 nM 7.62
CHEMBL5194202 IC50 = 39.0 nM 7.41
CHEMBL5182767 IC50 = 54.0 nM 7.27
CHEMBL5194833 IC50 = 127.0 nM 6.90
CHEMBL5187378 IC50 = 157.0 nM 6.80
CHEMBL5191136 IC50 = 179.0 nM 6.75