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Assay Detail

CHEMBL4611857

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

Binding
Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins followed by substrate and ATP addition
9
Total Activities
9
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

CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?
Diab S, Yu M, Wang S.
J Med Chem (2020) 63 : 7458 -7474
PubMed 32150405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3128043 PF-03758309 1.0 1 8.15
CHEMBL4434871 1 8.12
CHEMBL4450322 1 8.01
CHEMBL4303287 1 7.86
CHEMBL4436535 1 7.64
CHEMBL4582951 1 7.08
CHEMBL4441405 1 6.95
CHEMBL3603847 1 6.62
CHEMBL4163879 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3128043 PF-03758309 IC50 = 7.0 nM 8.15
CHEMBL4434871 IC50 = 7.6 nM 8.12
CHEMBL4450322 IC50 = 9.7 nM 8.01
CHEMBL4303287 IC50 = 13.9 nM 7.86
CHEMBL4436535 IC50 = 23.0 nM 7.64
CHEMBL4582951 IC50 = 84.0 nM 7.08
CHEMBL4441405 IC50 = 112.0 nM 6.95
CHEMBL3603847 IC50 = 238.0 nM 6.62
CHEMBL4163879 IC50 = 8500.0 nM 5.07