Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5717047

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

Binding
Inhibition of GST-tagged recombinant FLT3 D835Y mutant (unknown origin) expressed in baculovirus expression system using poly(Glu,Tyr) as substrate incubated for 2 hrs in presence of ATP by luminescence method
1
Total Activities
1
Compounds Tested
1
Activity Types
2
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

Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia.
Hart S, Goh KC, Novotny-Diermayr V, Tan YC, Madan B, Amalini C, Ong LC, Kheng B, Cheong A, Zhou J, Chng WJ, Wood JM.
Blood Cancer J (2011) 1
PubMed 22829080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.22 8.22

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000222
EFO_TERM EFO_TERM - acute myeloid leukemia

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035187 PACRITINIB 4.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035187 PACRITINIB IC50 = 6.0 nM 8.22