Activity-based RET-NCOA4 (PTC3) kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
-RET, NCOA4 (PTC3)
Enzyme
Human NCOA4-RET (PTC3) fusion
HGNC
RET-NCOA4
Synonym
CDHF12, CDHR16, HSCR1, MEN2A, MEN2B, MTC1, PTC, RET51
Substrates
Peptide substrate, [RRRRRRRRRRRVYSTDYYRLFNPS], 20 µM
ATP 10 µM
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| Staurosporine | 5.0 |
| PP2 | 27 |
| AG1478 | 330 |
| EGFR/ErbB Inhibitor | >100,000 |
| D-64406 | 160 |
Scientific Information
Screening Location
Malvern, USA
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