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Assay Detail

CHEMBL5043166

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

Binding
Inhibition of CDK12/cyclin K (unknown origin) using 5-FAM-labeled peptide as substrate in presence of ATP by mobility shift assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

CDK12/Cyclin K (CHEMBL4106169)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.
Marineau JJ, Hamman KB, Hu S, Alnemy S, Mihalich J, Kabro A, Whitmore KM, Winter DK, Roy S, Ciblat S, Ke N, Savinainen A, Wilsily A, Malojcic G, Zahler R, Schmidt D, Bradley MJ, Waters NJ, Chuaqui C.
J Med Chem (2022) 65 : 1458 -1480
PubMed 34726887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.10 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4791134 1 7.82
CHEMBL4786320 1 7.62
CHEMBL4555799 1 7.54
CHEMBL4782954 1 7.48
CHEMBL4786555 1 7.44
CHEMBL5083688 1 7.22
CHEMBL4779443 1 7.16
CHEMBL5088381 1 7.12
CHEMBL4786843 1 7.02
CHEMBL4786592 1 6.99
CHEMBL4790490 1 6.95
CHEMBL4800180 1 6.87
CHEMBL5080711 1 6.81
CHEMBL4798916 1 6.67
CHEMBL5090754 SY-5609 1.0 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4791134 IC50 = 15.0 nM 7.82
CHEMBL4786320 IC50 = 24.0 nM 7.62
CHEMBL4555799 IC50 = 29.0 nM 7.54
CHEMBL4782954 IC50 = 33.0 nM 7.48
CHEMBL4786555 IC50 = 36.0 nM 7.44
CHEMBL5083688 IC50 = 60.0 nM 7.22
CHEMBL4779443 IC50 = 69.0 nM 7.16
CHEMBL5088381 IC50 = 75.0 nM 7.12
CHEMBL4786843 IC50 = 95.0 nM 7.02
CHEMBL4786592 IC50 = 102.0 nM 6.99
CHEMBL4790490 IC50 = 112.0 nM 6.95
CHEMBL4800180 IC50 = 135.0 nM 6.87
CHEMBL5080711 IC50 = 156.0 nM 6.81
CHEMBL4798916 IC50 = 215.0 nM 6.67
CHEMBL5090754 SY-5609 IC50 = 1702.0 nM 5.77