Assay Detail

CHEMBL2327563

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Binding

Inhibition of c-MET Y1230H mutant (unknown origin)

ChEMBL ↗

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Target

Hepatocyte growth factor receptor (CHEMBL3717) ↗

Open DB target context

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Hepatocyte growth factor receptor (CHEMBL3717) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Hepatocyte growth factor receptor

CHEMBL3717

Anchored from Assay target.

Protein identity Hepatocyte growth factor receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Hepatocyte growth factor receptor (CHEMBL3717) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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	9.22	9.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2323775	MK-8033	1.0	1	9.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2323775	MK-8033	IC50	=	0.6	nM	9.22