Assay Detail

CHEMBL1804192

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Binding

Inhibition of human Flt3

ChEMBL ↗

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Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗

Open DB target context

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Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Receptor-type tyrosine-protein kinase FLT3

CHEMBL1974

Anchored from Assay target.

Protein identity Receptor-type tyrosine-protein kinase FLT3

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

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗

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
IC50	1	7.66	7.66

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1822792	MK-2461	2.0	1	7.66

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1822792	MK-2461	IC50	=	22.0	nM	7.66