Compound name
GSK579289A
Protein family
Protein Kinase
Target name
PLK1
Affinity biochemical (nM)
1
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001879a
SMILES
C[C@H](C1=C(C=CC=C1)Cl)OC2=C(SC(N3C4=CC(OC5CCN(CC5)C)=CC=C4N=C3)=C2)C(N)=O
InChIKey
GILNGUYOGYOZMP-MRXNPFEDSA-N
NCBI gene ID
5347
UniProt ID
P53350
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/19237286/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (DSF assay)
Selectivity platform number of targets
100
Selectivity remarks
Screened at 20 µM, clean profile, all targets dTm <5K;
Screened against 50 kinases, enzymatic assay, in-vitro potency of closest targets: IC50(PLK3) = 630 nM, IC50(PDGFR1B) = 420 nM, IC50(PIM1) = 310 nM, IC50(PI3KD) = 440 nM, IC50(VEGFR2) = 1200 nM, IC50(NUAK1) = 2000 nM, other kinases (not named) >1000 nM, https://pubmed.ncbi.nlm.nih.gov/19237286/;
Screened against 50 kinases, enzymatic assay, in-vitro potency of closest targets: IC50(PLK3) = 630 nM, IC50(PDGFR1B) = 420 nM, IC50(PIM1) = 310 nM, IC50(PI3KD) = 440 nM, IC50(VEGFR2) = 1200 nM, IC50(NUAK1) = 2000 nM, other kinases (not named) >1000 nM, https://pubmed.ncbi.nlm.nih.gov/19237286/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/19237286/
Selectivity Number of Off-targets
4