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Assay Detail

CHEMBL5043164

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

Binding
Binding affinity to full length CDK7 (1 to 346 residues) /N-terminal TEV cleavable 6His tagged full length cyclinH (1 to 323 residues) (unknown origin) expressed in baculovirus infected Sf9 cells by Surface plasmon resonance assay
15
Total Activities
15
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 7/ cyclin H (CHEMBL2111288)
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
Kd 15 9.93 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088381 1 10.52
CHEMBL5080711 1 10.22
CHEMBL4791134 1 10.15
CHEMBL5090754 SY-5609 1.0 1 10.15
CHEMBL4786592 1 10.10
CHEMBL4782954 1 10.10
CHEMBL5083688 1 10.05
CHEMBL4779443 1 10.00
CHEMBL4790490 1 10.00
CHEMBL4786320 1 9.82
CHEMBL4798916 1 9.82
CHEMBL4786555 1 9.68
CHEMBL4555799 1 9.48
CHEMBL4786843 1 9.47
CHEMBL4800180 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088381 Kd = 0.03 nM 10.52
CHEMBL5080711 Kd = 0.06 nM 10.22
CHEMBL4791134 Kd = 0.07 nM 10.15
CHEMBL5090754 SY-5609 Kd = 0.07 nM 10.15
CHEMBL4786592 Kd = 0.08 nM 10.10
CHEMBL4782954 Kd = 0.08 nM 10.10
CHEMBL5083688 Kd = 0.09 nM 10.05
CHEMBL4779443 Kd = 0.1 nM 10.00
CHEMBL4790490 Kd = 0.1 nM 10.00
CHEMBL4786320 Kd = 0.15 nM 9.82
CHEMBL4798916 Kd = 0.15 nM 9.82
CHEMBL4786555 Kd = 0.21 nM 9.68
CHEMBL4555799 Kd = 0.33 nM 9.48
CHEMBL4786843 Kd = 0.34 nM 9.47
CHEMBL4800180 Kd = 0.4 nM 9.40