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Assay Detail

CHEMBL2329607

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

Functional
In vivo inhibition of c-MET phosphorylation at tyrosine Y1349 in human GTL16 cells xenografted in po dosed mouse after 1 hr by Western blotting analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type GTL16
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ.
J Med Chem (2013) 56 : 2294 -2310
PubMed 23379595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.89 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2323775 MK-8033 1.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2323775 MK-8033 IC50 = 1300.0 nM 5.89