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Assay Detail

CHEMBL4132790

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

Binding
Inhibition of N-terminal GST tagged human PDGFRalpha (550 to 1089 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr by mobility shift assay
2
Total Activities
2
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

Platelet-derived growth factor receptor alpha (CHEMBL2007)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors.
Qin M, Tian Y, Sun X, Yu S, Xia J, Gong P, Zhang H, Zhao Y.
Eur J Med Chem (2017) 139 : 492 -502
PubMed 28826084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.50 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502835 NINTEDANIB 4.0 1 8.64
CHEMBL4165429 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502835 NINTEDANIB IC50 = 2.3 nM 8.64
CHEMBL4165429 IC50 = 4.4 nM 8.36