Compound name
LP-935509
Protein family
Protein Kinase
Target name
BIKE
Affinity biochemical (nM)
14
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002937a
SMILES
O=C(N1CCN(C2=NC3=C(C4=CC=CN=C4OC)C=NN3C=C2)CC1)OC(C)C
InChIKey
GOOYSJIWTIHOGW-UHFFFAOYSA-N
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Caliper enzyme assay (phosphorylation of peptide substrate, using 3.3 µM ATP = Km)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27411717/
Affinity biochemical relation
=
Selectivity platform
KINOMEscan (AMBIT/DiscoveRx)
Selectivity platform number of targets
389
Selectivity remarks
Screened at 1 µM, closest targets as % of control: AAK1 (2.1%), PRP4 (28%). RIOK1 (3.9%), RIOK3 (6.6%), BIKE (3.5%), SGK085 (7.6%), SGK288 (13%), SRPK1 (19%), SRPK2 (28%), LBK1 (9.7%), DRAK1 (6.4%), DRAK2 (30%), PIP5K2C (9.5%), full screening data arae available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 43 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(PDE4) = 8.3 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 8 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(α2A ) >1 µM, IC50(α2C) >1 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 43 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(PDE4) = 8.3 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 8 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(α2A ) >1 µM, IC50(α2C) >1 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27411717/
Selectivity Number of Off-targets
6