Synonyms: compound 1 [PMID 24044867] [1]
Compound class:
Synthetic organic
Comment: URMC-099 is an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3 (MLK3) and leucine-rich repeat kinase 2 (LRRK2) [1]. URMC-099 is being investigated as a lead compound with a novel mechanism of action for the treatment of Parkinson's disease and HIV-1 associated neurocognitive disorders (HAND).
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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Bioactivity Comments |
URMC-099 shows good brain penetrance and PK/PD dynamics in mice and exhibits activity in in vivo models of HAND [1]. Inhibition of FLT3 and LRRK2 may be involved in off-target neuroprotective effects of this compound. In a selectivity profile kinase screen >90% inhibition at 1μM was reported for ABL1, CDK11, CDK4, CDKL2, CLK1, CLK2, CLK4, DYRK1B, FLT3, KIT, MELK, PDGFRB, SRPK2, ALK, ARK5, AXL, IKKα, IKKβ, ROCK1 and TYK2. |
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Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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