Activity-based BMPR2 kinase assay for compound screening and profiling via Probe-Displacement kinase assay.
Target Overview
CAT#
BMPR2 (Binding)
Enzyme
Human BMPR2 (aa 189-529)
HGNC
BMPR2
Synonym
Bone morphogenetic protein receptor type-2, PPH1
Assay Properties
Probe
Fluorescent labeled ATP, 100 nM
Assay Format
Binding interaction between fluorescently labeled ATP and Kinase is quantified by HTRF technology using anti Tag HTRF reagents. Compounds binding in this binding pocket displace fluorescently labeled probe resulting loss of binding signal.
Readout
HTRF Readout, Probe-Displacement
Reference Compound IC50s
| Compounds | IC50 |
|---|---|
| CDD-1653 | 2.3 nM |
| BMPR2-IN-1 TFA | 66.6 nM |
| Staurosporine | 2.9 µM |
| ATP | 7.9 µM |
Scientific Information
Q13873 (http://www.uniprot.org/uniprot/Q13873)
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays
Reference compound inhibition of BMPR2
