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Assay Detail

CHEMBL5357372

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Binding
Inhibition of GST-tagged recombinant human CDK12 (696 to 1082 residues) expressed in Insect cell in presence of ATP by high ATP assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 12 (CHEMBL3559692)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Research progress of anticancer drugs targeting CDK12.
Yan Z, Du Y, Zhang H, Zheng Y, Lv H, Dong N, He F.
RSC Med Chem (2023) 14 : 1629 -1644
PubMed 37731700 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.88 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5414905 1 7.33
CHEMBL4649135 1 6.99
CHEMBL5188909 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5414905 IC50 = 47.0 nM 7.33
CHEMBL4649135 IC50 = 103.0 nM 6.99
CHEMBL5188909 IC50 = 491.0 nM 6.31