Assay Detail

CHEMBL1803997

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Binding

Binding affinity to human recombinant His6-tagged unphosphorylated c-Met cytosolic domain

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 a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q.
J Med Chem (2011) 54 : 4092 -4108
PubMed 21608528 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	7.60	7.60

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1822792	MK-2461	2.0	1	7.60

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1822792	MK-2461	Kd	=	25.0	nM	7.60