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

CHEMBL1244848

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

Binding
Binding affinity to FLT3 ITD mutant
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
Kd 7 8.05 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 9.00
CHEMBL603469 LESTAURTINIB 3.0 1 8.82
CHEMBL576982 QUIZARTINIB 4.0 1 8.06
CHEMBL124660 TANDUTINIB 2.0 1 8.04
CHEMBL608533 MIDOSTAURIN 4.0 1 7.96
CHEMBL1240703 CGP-52421 1 7.37
CHEMBL1336 SORAFENIB 4.0 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 0.99 nM 9.00
CHEMBL603469 LESTAURTINIB Kd = 1.5 nM 8.82
CHEMBL576982 QUIZARTINIB Kd = 8.8 nM 8.06
CHEMBL124660 TANDUTINIB Kd = 9.1 nM 8.04
CHEMBL608533 MIDOSTAURIN Kd = 11.0 nM 7.96
CHEMBL1240703 CGP-52421 Kd = 43.0 nM 7.37
CHEMBL1336 SORAFENIB Kd = 79.0 nM 7.10