Activity-based RET kinase assay for compound screening and profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
RET
Enzyme
Human RET
HGNC
RET
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 | 7.1 |
| PP2 | 24 |
| AG1478 | 260 |
| EGFR/ErbB Inhibitor | >100,000 |
| D-64406 | 104 |
Scientific Information
P07949 (http://www.uniprot.org/uniprot/P07949)
Screening Location
Malvern, USA
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