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Assay Detail

CHEMBL5609520

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

Binding
Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay
23
Total Activities
23
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

CDK7/Cyclin H/MNAT1 (CHEMBL3038473)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).
Ji W, Du G, Jiang J, Lu W, Mills CE, Yuan L, Jiang F, He Z, Bradshaw GA, Chung M, Jiang Z, Byun WS, Hinshaw SM, Zhang T, Gray NS.
Eur J Med Chem (2024) 276 : 116613 -116613
PubMed 39004018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.91 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5612636 1 8.25
CHEMBL5613276 1 8.19
CHEMBL5613200 1 8.17
CHEMBL5613393 1 8.16
CHEMBL5612049 1 8.12
CHEMBL5612354 1 8.11
CHEMBL5613342 1 8.09
CHEMBL5611964 1 8.07
CHEMBL5613703 1 8.06
CHEMBL5613991 1 8.04
CHEMBL5612986 1 8.03
CHEMBL5613579 1 7.96
CHEMBL5612749 1 7.95
CHEMBL5613917 1 7.92
CHEMBL5613656 1 7.90
CHEMBL5612598 1 7.88
CHEMBL5612241 1 7.87
CHEMBL5613012 1 7.86
CHEMBL5614037 1 7.75
CHEMBL5612001 1 7.70
CHEMBL5613124 1 7.68
CHEMBL5612073 1 7.46
CHEMBL5612364 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5612636 IC50 = 5.6 nM 8.25
CHEMBL5613276 IC50 = 6.4 nM 8.19
CHEMBL5613200 IC50 = 6.7 nM 8.17
CHEMBL5613393 IC50 = 6.9 nM 8.16
CHEMBL5612049 IC50 = 7.6 nM 8.12
CHEMBL5612354 IC50 = 7.8 nM 8.11
CHEMBL5613342 IC50 = 8.1 nM 8.09
CHEMBL5611964 IC50 = 8.6 nM 8.07
CHEMBL5613703 IC50 = 8.7 nM 8.06
CHEMBL5613991 IC50 = 9.2 nM 8.04
CHEMBL5612986 IC50 = 9.4 nM 8.03
CHEMBL5613579 IC50 = 11.1 nM 7.96
CHEMBL5612749 IC50 = 11.3 nM 7.95
CHEMBL5613917 IC50 = 12.1 nM 7.92
CHEMBL5613656 IC50 = 12.6 nM 7.90
CHEMBL5612598 IC50 = 13.3 nM 7.88
CHEMBL5612241 IC50 = 13.4 nM 7.87
CHEMBL5613012 IC50 = 13.7 nM 7.86
CHEMBL5614037 IC50 = 17.7 nM 7.75
CHEMBL5612001 IC50 = 20.1 nM 7.70
CHEMBL5613124 IC50 = 21.1 nM 7.68
CHEMBL5612073 IC50 = 34.4 nM 7.46
CHEMBL5612364 IC50 = 203.0 nM 6.69