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 [4].
Cereblon-targeting LRRK2 PROTACs have been disclosed previously, but these were found to be inefficient target degraders [3]. |
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Classification | |
Compound class | Synthetic organic |
Ligand families/groups | PROTACs, molecular glues and other degraders |
Database Links | |
GtoPdb PubChem SID | 464244150 |
PubChem CID | 163358787 |
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 |