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Assay Detail

CHEMBL3707574

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

Binding
Kinase Assay: The effect of test compounds on the activity of the protein kinases GSK-3β, VEGFR-2 and FLT-3 was evaluated based on half maximal inhibitory concentration (IC50) values determined by Millipore UK Ltd; Gemini Crescent; Dundee Technology Park; Dundee DD2 1SW; UK (IC50Profiler). Detailed protocols can be found at: www.millipore.com/drugdiscovery/dd3/assayprotocols.
6
Total Activities
5
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

Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.40 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3699444 1 6.62
CHEMBL201511 MALEIMIDE 1 6.57
CHEMBL3699443 1 6.32
CHEMBL3699446 2 6.26
CHEMBL3699445 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3699444 IC50 = 239.0 nM 6.62
CHEMBL201511 MALEIMIDE IC50 = 270.0 nM 6.57
CHEMBL3699443 IC50 = 480.0 nM 6.32
CHEMBL3699446 IC50 = 554.0 nM 6.26
CHEMBL3699446 IC50 = 556.0 nM 6.25
CHEMBL3699445 IC50 > 1000.0 nM -