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Assay Detail

CHEMBL1244699

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

Functional
Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Autocuration

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS.
Blood (2009) 114 : 2984 -2992
PubMed 19654408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.24 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576982 QUIZARTINIB 4.0 1 9.25
CHEMBL1336 SORAFENIB 4.0 1 9.06
CHEMBL603469 LESTAURTINIB 3.0 1 8.68
CHEMBL535 SUNITINIB 4.0 1 8.37
CHEMBL608533 MIDOSTAURIN 4.0 1 7.92
CHEMBL124660 TANDUTINIB 2.0 1 7.22
CHEMBL1240703 CGP-52421 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576982 QUIZARTINIB IC50 = 0.56 nM 9.25
CHEMBL1336 SORAFENIB IC50 = 0.87 nM 9.06
CHEMBL603469 LESTAURTINIB IC50 = 2.1 nM 8.68
CHEMBL535 SUNITINIB IC50 = 4.3 nM 8.37
CHEMBL608533 MIDOSTAURIN IC50 = 12.0 nM 7.92
CHEMBL124660 TANDUTINIB IC50 = 60.0 nM 7.22
CHEMBL1240703 CGP-52421 IC50 = 64.0 nM 7.19