Compound name
LP-935509
Protein family
Protein Kinase
Target name
AAK1
Affinity biochemical (nM)
3.3
Affinity on-target cellular (nM)
2.8
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
NCBI gene ID
22848
UniProt ID
Q2M2I8
Synonyms
KIAA1048, DKFZp686K16132
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Caliper enzyme assay (phosphorylation of peptide substrate, using 22 µM ATP = Km)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27411717/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (inhibition of MU-2 phosphorylation using HEK293 cells with adaptor protein 2 (AP-2))
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/27411717/
Affinity on-target cellular 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