Compound name
HG-10-102-01
Protein family
Protein Kinase
Target name
LRRK2
Affinity biochemical (nM)
20.3
Affinity on-target cellular (nM)
1000
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001264a
SMILES
CNc1nc(Nc2ccc(C(=O)N3CCOCC3)cc2OC)ncc1Cl
InChIKey
YEVOZZZLKJKCCD-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
Enzymatic assay (using 0.1 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23066449/
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Immunoblot assay (dephosphorylation of pS910 using HEK293 cells stably expressing wild-type GFP-LRRK2)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/23066449/
Affinity on-target cellular relation
<
Selectivity platform
Kinase panel (Dundee profiling)
Selectivity platform number of targets
138
Selectivity remarks
Screened at 1 µM nd 10 µM, closest targets as % of control at 1 µM: MAP3K7 (16%), MST2 (17%), BRSK1 (18%), MAP2K2 (17%), ERK1 (16%), full screening data available as supplemental information; Screened at 1 µM against 451 kinases (KinomeScan, DiscoverX), closest targets as % of control: KIT (L576P, 9.4%), LRRK2 (G2019S, 2.1%), others >10%, full screening data available as supporting information,https://pubmed.ncbi.nlm.nih.gov/23066449/; Screened in KiNativ Profiling in tissue from inhibitor-treated animals, closest targets JNK1/2/3 and TBK1 potential dose-related inhibition (∼35–40% at 50 and 100 mg/kg), full screening data available as supporting information,https://pubmed.ncbi.nlm.nih.gov/23066449/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23066449/
Selectivity Number of Off-targets
0