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Assay Detail

CHEMBL3779075

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

Binding
Inhibition of CDK8-mediated STAT1 phosphorylation at serine727 in human SW620 cells harboring APC mutant
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SW-620
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 8 (CHEMBL5719)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.
Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.
Bioorg Med Chem Lett (2016) 26 : 1443 -1451
PubMed 26852363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.31 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775576 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775576 IC50 = 49.0 nM 7.31