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Assay Detail

CHEMBL4701739

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Binding
Inhibition of FLT3 ITD/D835Y double mutant (unknown origin) expressed in mouse BaF3 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
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 small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.
Zhang G,Zhang W,Shen C,Nan J,Chen M,Lai S,Zhong J,Li B,Wang T,Wang Y,Yang S,Li L
Bioorg Med Chem Lett (2020) 30 : 127532 -127532
PubMed 32891702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.52 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790915 1 8.46
CHEMBL4765203 1 8.29
CHEMBL4763828 1 8.27
CHEMBL4795857 1 8.22
CHEMBL4749484 1 8.20
CHEMBL4781811 1 8.10
CHEMBL4791482 1 8.00
CHEMBL4782974 1 7.97
CHEMBL4750430 1 7.96
CHEMBL4765096 1 7.96
CHEMBL4744130 1 7.91
CHEMBL4780418 1 7.83
CHEMBL4763034 1 7.81
CHEMBL4755159 1 7.55
CHEMBL4749639 1 7.46
CHEMBL4757207 1 7.21
CHEMBL4761091 1 7.19
CHEMBL4798245 1 6.98
CHEMBL4519741 1 6.89
CHEMBL4793076 1 6.80
CHEMBL576982 QUIZARTINIB 4.0 1 6.28
CHEMBL4749438 1 6.13
CHEMBL4800630 1 5.45
CHEMBL4744221 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790915 IC50 = 3.48 nM 8.46
CHEMBL4765203 IC50 = 5.09 nM 8.29
CHEMBL4763828 IC50 = 5.35 nM 8.27
CHEMBL4795857 IC50 = 5.96 nM 8.22
CHEMBL4749484 IC50 = 6.28 nM 8.20
CHEMBL4781811 IC50 = 7.93 nM 8.10
CHEMBL4791482 IC50 = 10.1 nM 8.00
CHEMBL4782974 IC50 = 10.6 nM 7.97
CHEMBL4750430 IC50 = 11.0 nM 7.96
CHEMBL4765096 IC50 = 10.9 nM 7.96
CHEMBL4744130 IC50 = 12.4 nM 7.91
CHEMBL4780418 IC50 = 14.9 nM 7.83
CHEMBL4763034 IC50 = 15.5 nM 7.81
CHEMBL4755159 IC50 = 27.9 nM 7.55
CHEMBL4749639 IC50 = 34.3 nM 7.46
CHEMBL4757207 IC50 = 62.4 nM 7.21
CHEMBL4761091 IC50 = 64.2 nM 7.19
CHEMBL4798245 IC50 = 104.0 nM 6.98
CHEMBL4519741 IC50 = 130.0 nM 6.89
CHEMBL4793076 IC50 = 160.0 nM 6.80
CHEMBL576982 QUIZARTINIB IC50 = 520.0 nM 6.28
CHEMBL4749438 IC50 = 741.1 nM 6.13
CHEMBL4800630 IC50 = 3540.8 nM 5.45
CHEMBL4744221 IC50 > 10000.0 nM -