Compound name
PF-06447475
Protein family
Protein Kinase
Target name
LRRK2
Affinity biochemical (nM)
3
Affinity on-target cellular (nM)
84
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
120892
UniProt ID
Q5S007
Synonyms
ROCO2, DKFZp434H2111, FLJ45829, RIPK7
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Lanthascreen assay (Invitrogen, using 117 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