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Assay Detail

CHEMBL4401401

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

Binding
Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system preincubated for 5 to 30 mins followed by myelobasic protein addition measured after 120 mins in presence of ATP by ADP-Glo assay
2
Total Activities
2
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
Ki 2 8.35 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553725 1 8.70
CHEMBL4442997 1 7.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553725 Ki = 1.98 nM 8.70
CHEMBL4442997 Ki = 10.14 nM 7.99