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Compound class: Synthetic organic
Comment: XL01126 is a VHL-based PROTAC degrader targeting leucine rich repeat kinase 2 (LRRK2). The LRRK2 binding moeity of the compound is the brain-penetrant kinase inhibitor HG-10-102-01. XL01126 is orally bioavailable and retains the ability of the parent kinase inhibitor to cross the blood-brain barrier. LRRK2 is an active therapeutic target for Parkinson's disease, since activating coding mutations in LRRK2 are associated with dominantly inherited Parkinson's disease [1-2,5]. XL01126's development was led by Dundee University's Centre for Targeted Protein Degradation and the Research Institute for Medicines at the University of Lisbon. Initially disclosed in a ChemRxiv preprint .
Cereblon-targeting LRRK2 PROTACs have been disclosed previously, but these were found to be inefficient target degraders .
|Compound class||Synthetic organic|
|Ligand families/groups||PROTACs, molecular glues and other degraders|
|GtoPdb PubChem SID||464244150|
|Search Google for chemical match using the InChIKey||XSOATTNBVDAEAR-QGHWPEOCSA-N|
|Search Google for chemicals with the same backbone||XSOATTNBVDAEAR|
|UniChem Compound Search for chemical match using the InChIKey||XSOATTNBVDAEAR-QGHWPEOCSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||XSOATTNBVDAEAR-QGHWPEOCSA-N|