Compound name
XL413
Protein family
Protein Kinase
Target name
PIM1
Affinity biochemical (nM)
42
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0003007aCl
SMILES
O=C1C2=C(N=C(N1)[C@@H]3CCCN3)C4=CC(Cl)=CC=C4O2.[H]Cl
InChIKey
JJWLXRKVUJDJKG-VIFPVBQESA-N
NCBI gene ID
5292
UniProt ID
P11309
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Luciferase-luciferin-coupled chemiluminescence assay (using 0.5 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22560567/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Proteomica, Kinobead assay)
Selectivity platform number of targets
263
Selectivity remarks
Screened in competition binding assays usisng K-562, COLO 205, SK-N-BE(2) and MV-4-11 cell lysates, in-vitro potency of closest targets: Kd(DYRK1A) = 40 nM, Kd(CSNK2A1) = 22 nM, Kd(PIM1) = 22 nM, Kd(TAO3) = 2292 nM, Kd(CIT) = 3659 nM, Kd(GSK3B) = 8793 nM, all other targets Kd >3000 nM, full screening data are available at Chembl;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/29191878/
Selectivity Number of Off-targets
2