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Assay Detail

CHEMBL3829704

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

Functional
In vivo inhibition of STAT1 phosphorylation at ser727 in human SW620 cells harboring APC mutation xenografted in mouse administered through oral gavage every 24 hrs measured after 2 to 24 hrs post last dose by Western blot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type SW-620
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J.
ACS Med Chem Lett (2016) 7 : 573 -578
PubMed 27326329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.35 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828553 1 7.75
CHEMBL3827758 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828553 IC50 = 17.9 nM 7.75
CHEMBL3827758 IC50 = 114.0 nM 6.94