Synonyms: compound 15 [PMID: 22591441]
Compound class:
Synthetic organic
Comment: HG-10-102-01 is a brain-penetrant, selective small-molecule inhibitor of LRRK2 (leucine rich repeat kinase 2), activating mutations of which have been associated with Parkinson's disease [1]. An alternative stereoisomer is presented in [2].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Chen H, Chan BK, Drummond J, Estrada AA, Gunzner-Toste J, Liu X, Liu Y, Moffat J, Shore D, Sweeney ZK et al.. (2012)
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling. J Med Chem, 55 (11): 5536-45. [PMID:22591441] |
2. Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. (2012)
Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett, 3 (8): 658-662. [PMID:23066449] |
3. Liu X, Kalogeropulou K, Domingos S, Makukhin N, Nirujogi R, Singh F, Shpiro N, Saalfrank A, Sammler E, Ganley I et al.. (2022)
Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Oral bioavailable and Blood Brain Barrier Penetrant PROTAC Degrader of Leucine Rich Repeat Kinase 2 (LRRK2). chemrxiv, Preprint. DOI: 10.26434/chemrxiv-2022-4gzm0 |