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Assay Detail

CHEMBL4031419

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

Binding
Inhibition of GST-tagged human DDR2 (427 to 855 residues) expressed in Baculovirus expression system by Z'Lyte assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Discoidin domain-containing receptor 2 (CHEMBL5122)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Wang A, Li X, Chen C, Wu H, Qi Z, Hu C, Yu K, Wu J, Liu J, Liu X, Hu Z, Wang W, Wang W, Wang W, Wang L, Wang B, Liu Q, Li L, Ge J, Ren T, Zhang S, Xia R, Liu J, Liu Q.
J Med Chem (2017) 60 : 8407 -8424
PubMed 28956923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.21 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101411 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101411 IC50 = 61.0 nM 7.21