Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.

Bioorganic & medicinal chemistry letters - 1 Sept 2012

Reith Alastair D, Bamborough Paul, Jandu Karamjit, Andreotti Daniele, Mensah Lucy, Dossang Pamela, Choi Hwan Geun, Deng Xianming, Zhang Jinwei, Alessi Dario R, Gray Nathanael S

Abstract excerpt

Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for some forms of Parkinson's disease. Here we report the discovery and characterization of 2-arylmethyloxy-5-subtitutent-N-arylbenzamides with potent LRRK2 activities exemplified by GSK2578215A which exhibits biochemical IC(50)s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to 3T3 Cells
Share to Drug Discovery

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to HEK293 Cells

Share to Leucine-Rich Repeat Serine-Threonine Protein Kinase-2

Share to Parkinson Disease

Share to Protein Kinase Inhibitors

Share to Protein Serine-Threonine Kinases

Share to Structural Homology, Protein

Source

Open in PubMed Open full text

Identifiers

PMID: 22863203
DOI: 10.1016/j.bmcl.2012.06.104
PMCID: PMC4208292

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.PMID 22863203Read ↗

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.Semantic proximity Read ↗

Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.Semantic proximity Read ↗

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.Semantic proximity Read ↗

MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.Semantic proximity Read ↗

Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy.Semantic proximity Read ↗

Selective Inhibitors of G2019S-LRRK2 Kinase Activity.Semantic proximity Read ↗

Discovery of Highly Potent, Selective, and Brain-Penetrant Aminopyrazole Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule InhibitorsSemantic proximity Read ↗

Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase InhibitorsSemantic proximity Read ↗

Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).Semantic proximity Read ↗

Leucine-rich repeat kinase 2 inhibitors: a review of recent patents (2011 – 2013)Semantic proximity Read ↗

Discovery of Highly Potent, Selective, and Brain-Penetrable Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule InhibitorsSemantic proximity Read ↗

Recent advances in targeting leucine-rich repeat kinase 2 as a potential strategy for the treatment of Parkinson's disease.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.