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Assay Detail

CHEMBL3270317

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

Binding
Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MV4-11
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 GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA.
J Med Chem (2014) 57 : 3856 -3873
PubMed 24779514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.25 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475251 R-406 2.0 1 8.00
CHEMBL3265032 ENTOSPLETINIB 3.0 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475251 R-406 EC50 = 10.0 nM 8.00
CHEMBL3265032 ENTOSPLETINIB EC50 = 327.0 nM 6.49