EUB0001619a_STK3

Chemical structure of compound EUB0001619a
Compound name
PF-06447475
Protein family
Protein Kinase
Target name
STK3
Affinity biochemical (nM)
22
Affinity on-target cellular (nM)
197
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001619a
SMILES
N#Cc1cccc(-c2c[nH]c3ncnc(N4CCOCC4)c23)c1
InChIKey
BHTWDJBVZQBRKP-UHFFFAOYSA-N
NCBI gene ID
6788
UniProt ID
Q13188
Synonyms
MST2, KRS1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Z-Lyte assay assay (Invitrogen, using 7.75 µM ATP)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/jm5014055
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/epdf/10.1021/acs.jmedchem.1c00804
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
360
Selectivity remarks
Screened at 1 µM, closest targets as % of contr: MAP3K3(8.2%), MAP4K2(3.4%), JAK3(2.7%), MST2(1.8%), MAP4K3(4.8%), RIOK3(4.8%), RSK4(9.8%), MST4(7%), PRKCE(12%), MEK1(13%), EGFR(L747-E749del, 14%), EGFR(L747-S752del,14%), MEK5(14%), MEST1(18%), MEK2(19%), PIP5K1A(20%); In-vitro potency of closest targets (Z-Lyte assay assay, Invitrogen, using 7.75 µM ATP): IC50(MST4) = 178 nM, https://pubs.acs.org/doi/10.1021/jm5014055;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/jm5014055