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Assay Detail

CHEMBL5371159

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

Functional
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.
Zhi Y, Li H, Yang P, Jin Q, Yao C, Li B, Ling J, Guo H, Li T, Jin J, Wang Y, Chen Y, Lu T, Lu S.
Eur J Med Chem (2023) 256 : 115448 -115448
PubMed 37163951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.33 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL608533 MIDOSTAURIN 4.0 1 8.15
CHEMBL4077071 1 7.25
CHEMBL5401158 1 7.02
CHEMBL576982 QUIZARTINIB 4.0 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL608533 MIDOSTAURIN IC50 = 7.0 nM 8.15
CHEMBL4077071 IC50 = 56.0 nM 7.25
CHEMBL5401158 IC50 = 95.0 nM 7.02
CHEMBL576982 QUIZARTINIB IC50 = 133.0 nM 6.88