Activity-based PDGFRa kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
PDGFRα
Enzyme
Human PDGFRα
HGNC
PDGFRA
Synonym
PDGFR2, CD140a
Substrates
Peptide substrate, poly[Glu:Tyr] (4:1), 0.1 mg/ml
ATP 10 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | <0.1 |
| PP2 | 18.9 |
| AG1478 | 306 |
| PDGFR I-III | 2.4 |
| D-64406 | 453 |
Scientific Information
Q9DE49 (http://www.uniprot.org/uniprot/Q9DE49)
Screening Location
Malvern, USA
Reference compound IC50 for PDGFRα
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