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Assay Detail

CHEMBL4337765

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

Binding
Inhibition of human FLT3 using EAIYAAPFAKKK substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
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

Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
Han Y, Sengupta S, Lee BJ, Cho H, Kim J, Choi HG, Dash U, Kim JH, Kim ND, Kim JH, Sim T.
J Med Chem (2019) 62 : 9141 -9160
PubMed 31513411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.78 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012519 1 8.74
CHEMBL4453304 1 8.36
CHEMBL4515000 1 7.77
CHEMBL4533447 1 7.39
CHEMBL4452766 1 6.96
CHEMBL4303275 1 6.54
CHEMBL4515912 1 6.43
CHEMBL4438318 1 5.34
CHEMBL4517550 1 5.13
CHEMBL4572320 1 5.11
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL4530473 1 -
CHEMBL4520759 1 -
CHEMBL4471009 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012519 IC50 = 1.8 nM 8.74
CHEMBL4453304 IC50 = 4.37 nM 8.36
CHEMBL4515000 IC50 = 17.0 nM 7.77
CHEMBL4533447 IC50 = 41.0 nM 7.39
CHEMBL4452766 IC50 = 110.0 nM 6.96
CHEMBL4303275 IC50 = 290.0 nM 6.54
CHEMBL4515912 IC50 = 370.0 nM 6.43
CHEMBL4438318 IC50 = 4530.0 nM 5.34
CHEMBL4517550 IC50 = 7393.0 nM 5.13
CHEMBL4572320 IC50 = 7800.0 nM 5.11
CHEMBL576982 QUIZARTINIB IC50 < 0.51 nM -
CHEMBL4530473 IC50 - -
CHEMBL4520759 IC50 - -
CHEMBL4471009 IC50 - -