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Assay Detail

CHEMBL4401423

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Binding
Binding affinity to human FLT3 ITD/D835V double mutant expressed in baculovirus expression system
7
Total Activities
7
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

Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
Bensinger D, Stubba D, Cremer A, Kohl V, Waßmer T, Stuckert J, Engemann V, Stegmaier K, Schmitz K, Schmidt B.
J Med Chem (2019) 62 : 2428 -2446
PubMed 30742435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.64 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553725 1 9.08
CHEMBL1336 SORAFENIB 4.0 1 6.20
CHEMBL535 SUNITINIB 4.0 1 -
CHEMBL2105728 CRENOLANIB 3.0 1 -
CHEMBL608533 MIDOSTAURIN 4.0 1 -
CHEMBL576982 QUIZARTINIB 4.0 1 -
CHEMBL572878 TOZASERTIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553725 Kd = 0.83 nM 9.08
CHEMBL1336 SORAFENIB Kd = 630.0 nM 6.20
CHEMBL535 SUNITINIB Kd - -
CHEMBL2105728 CRENOLANIB Kd - -
CHEMBL608533 MIDOSTAURIN Kd - -
CHEMBL576982 QUIZARTINIB Kd - -
CHEMBL572878 TOZASERTIB Kd - -