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Assay Detail

CHEMBL4806367

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

Binding
Inhibition of CDK8/CDK19 in HEK293 cells by NF-kappaB reporter assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 8/19 (CHEMBL3885556)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

3-amino-4-(4-(4 (dimethylcarbamoyl) phenyl)-1,4-diazepan-1-yl) thieno [2,3-b] pyridine-2-carboxamide for use in cancer therapy and formulations comprising the same
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.69 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2348353 1 8.40
CHEMBL2348350 1 8.00
CHEMBL2348351 1 7.64
CHEMBL2348342 1 7.42
CHEMBL2348345 1 7.37
CHEMBL2348339 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2348353 IC50 = 4.0 nM 8.40
CHEMBL2348350 IC50 = 10.0 nM 8.00
CHEMBL2348351 IC50 = 23.1 nM 7.64
CHEMBL2348342 IC50 = 37.8 nM 7.42
CHEMBL2348345 IC50 = 43.1 nM 7.37
CHEMBL2348339 IC50 = 50.6 nM 7.30