Compound name
GSK579289A
Protein family
Protein Kinase
Target name
NEK2
Affinity biochemical (nM)
21
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
4751
UniProt ID
P51955
Synonyms
NLK1, NEK2A, RP67, PPP1R111
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