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Assay Detail

CHEMBL957979

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

Binding
Inhibition of human recombinant FLT3
12
Total Activities
12
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

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schächtele C, Heidenreich R, Röcken M, Schollmeyer D, Laufer S.
J Med Chem (2008) 51 : 3814 -3824
PubMed 18529047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.06 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201511 MALEIMIDE 1 6.57
CHEMBL521201 1 5.66
CHEMBL453593 1 5.52
CHEMBL509435 1 5.30
CHEMBL529663 1 5.21
CHEMBL452812 1 5.00
CHEMBL507056 1 4.85
CHEMBL488646 1 4.70
CHEMBL519590 1 4.60
CHEMBL486437 1 4.47
CHEMBL453336 1 4.44
CHEMBL505253 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201511 MALEIMIDE IC50 = 270.0 nM 6.57
CHEMBL521201 IC50 = 2200.0 nM 5.66
CHEMBL453593 IC50 = 3000.0 nM 5.52
CHEMBL509435 IC50 = 5000.0 nM 5.30
CHEMBL529663 IC50 = 6100.0 nM 5.21
CHEMBL452812 IC50 = 9900.0 nM 5.00
CHEMBL507056 IC50 = 14000.0 nM 4.85
CHEMBL488646 IC50 = 20000.0 nM 4.70
CHEMBL519590 IC50 = 25000.0 nM 4.60
CHEMBL486437 IC50 = 34000.0 nM 4.47
CHEMBL453336 IC50 = 36000.0 nM 4.44
CHEMBL505253 IC50 = 44000.0 nM 4.36