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Assay Detail

CHEMBL5717698

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

Binding
Inhibition of CDK2/Cyclin A (unknown origin) using ULight MBP peptide as substrate in presence of ATP incubated for 1 hr by FRET based LANCE Ultra KinaSelect screen assay
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor.
Albert TK, Rigault C, Eickhoff J, Baumgart K, Antrecht C, Klebl B, Mittler G, Meisterernst M.
Br J Pharmacol (2014) 171 : 55 -68
PubMed 24102143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.22 8.22

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000095
EFO_TERM EFO_TERM - chronic lymphocytic leukemia

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296468 BMS-387032 1.0 1 8.22
CHEMBL428690 ALVOCIDIB 3.0 1 7.82
CHEMBL5722954 1 5.61
CHEMBL375530 DICHLORORIBOBENZIMIDAZOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296468 BMS-387032 IC50 = 6.0 nM 8.22
CHEMBL428690 ALVOCIDIB IC50 = 15.0 nM 7.82
CHEMBL5722954 IC50 = 2441.0 nM 5.61
CHEMBL375530 DICHLORORIBOBENZIMIDAZOLE IC50 > 10000.0 nM -