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Assay Detail

CHEMBL1244559

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

Binding
Binding affinity to PDGFRB
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
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
Kd 7 7.88 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 10.12
CHEMBL124660 TANDUTINIB 2.0 1 8.35
CHEMBL576982 QUIZARTINIB 4.0 1 8.11
CHEMBL603469 LESTAURTINIB 3.0 1 7.55
CHEMBL1336 SORAFENIB 4.0 1 7.43
CHEMBL1240703 CGP-52421 1 7.17
CHEMBL608533 MIDOSTAURIN 4.0 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 0.075 nM 10.12
CHEMBL124660 TANDUTINIB Kd = 4.5 nM 8.35
CHEMBL576982 QUIZARTINIB Kd = 7.7 nM 8.11
CHEMBL603469 LESTAURTINIB Kd = 28.0 nM 7.55
CHEMBL1336 SORAFENIB Kd = 37.0 nM 7.43
CHEMBL1240703 CGP-52421 Kd = 68.0 nM 7.17
CHEMBL608533 MIDOSTAURIN Kd = 380.0 nM 6.42