Compound name
GW843682X
Protein family
Protein Kinase
Target name
PLK1
Affinity biochemical (nM)
2.2
Affinity on-target cellular (nM)
140
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000698a
SMILES
COC1=C(OC)C=C(N=CN2C3=CC(OCC4=CC=CC=C4C(F)(F)F)=C(C(N)=O)S3)C2=C1
InChIKey
JSKUWFIZUALZLX-UHFFFAOYSA-N
NCBI gene ID
5347
UniProt ID
P53350
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/7267659/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (PLK1 phosphorylation of Ser15-p53 in HeLa cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
441
Selectivity remarks
Screened at 10 µM, closest targets as % of contr.: GAK(4.1%), RIOK1/3 (4.1/4.2%), PDGFRB (5.3%), FLT3(D835H)(1.4%), FLT4(1.4%), KIT(D816V)(1.4%), PIP5K2B(6.6%), MAPK3K1(1.6%), PIP5K2B(6.6%), DAPK1(8.6%), FLT3(N841I) (1.7%), ROCK1 (4.7%), MST2(1.8%), SRPK1(8.9%), EPHB6(9.9%), LOK(0.0%), PLK2(0.2%), SLK(0.3%), MP2K5(0.5%), BIKE(1.0%), PIP5K1C (10%); Screened against 30 kinases, closest targets: IC50(PDGFR1b) = 160 nM, IC50(VEGFR2) = 360 nM, IC50(AURA) = 4800 nM, IC50(CDK2/cyclinA) = 7600 nM, others IC50 >10 µM (PMID: 17267659)
Selectivity Source Knowledge
https://lincs.hms.harvard.edu/db/datasets/20032/main
Selectivity Number of Off-targets
22