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Assay Detail

CHEMBL3385423

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

Binding
Inhibition of recombinant FLT3 D835Y mutant (unknown origin) by TR-FRET assay
27
Total Activities
27
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 FLT3 covalent inhibitors with a resorcylic acid core.
Xu J, Ong EH, Hill J, Chen A, Chai CL.
Bioorg Med Chem (2014) 22 : 6625 -6637
PubMed 25456387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.59 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012519 1 7.96
CHEMBL3357191 1 6.09
CHEMBL3357190 1 6.03
CHEMBL3357193 1 6.02
CHEMBL3357188 1 5.87
CHEMBL3357192 1 5.76
CHEMBL3357194 1 5.68
CHEMBL3357177 1 5.55
CHEMBL3357189 1 5.52
CHEMBL3357187 1 5.44
CHEMBL3357195 1 5.28
CHEMBL3357178 1 4.98
CHEMBL3357181 1 4.92
CHEMBL3357196 1 4.85
CHEMBL3357179 1 4.80
CHEMBL3357182 1 4.73
CHEMBL3357200 1 -
CHEMBL3357199 1 -
CHEMBL3357198 1 -
CHEMBL3357197 1 -
CHEMBL3357175 1 -
CHEMBL3357186 1 -
CHEMBL3357185 1 -
CHEMBL3357184 1 -
CHEMBL3357183 1 -
CHEMBL3357176 1 -
CHEMBL3357180 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012519 IC50 = 11.0 nM 7.96
CHEMBL3357191 IC50 = 810.0 nM 6.09
CHEMBL3357190 IC50 = 940.0 nM 6.03
CHEMBL3357193 IC50 = 950.0 nM 6.02
CHEMBL3357188 IC50 = 1340.0 nM 5.87
CHEMBL3357192 IC50 = 1740.0 nM 5.76
CHEMBL3357194 IC50 = 2100.0 nM 5.68
CHEMBL3357177 IC50 = 2810.0 nM 5.55
CHEMBL3357189 IC50 = 3030.0 nM 5.52
CHEMBL3357187 IC50 = 3610.0 nM 5.44
CHEMBL3357195 IC50 = 5200.0 nM 5.28
CHEMBL3357178 IC50 = 10520.0 nM 4.98
CHEMBL3357181 IC50 = 12030.0 nM 4.92
CHEMBL3357196 IC50 = 14150.0 nM 4.85
CHEMBL3357179 IC50 = 15900.0 nM 4.80
CHEMBL3357182 IC50 = 18590.0 nM 4.73
CHEMBL3357200 IC50 >= 30000.0 nM -
CHEMBL3357199 IC50 >= 30000.0 nM -
CHEMBL3357198 IC50 >= 30000.0 nM -
CHEMBL3357197 IC50 >= 30000.0 nM -
CHEMBL3357175 IC50 >= 30000.0 nM -
CHEMBL3357186 IC50 >= 30000.0 nM -
CHEMBL3357185 IC50 >= 30000.0 nM -
CHEMBL3357184 IC50 >= 30000.0 nM -
CHEMBL3357183 IC50 >= 30000.0 nM -
CHEMBL3357176 IC50 > 30000.0 nM -
CHEMBL3357180 IC50 > 30000.0 nM -