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GSK2578215A

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

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 17, 2012, p. 5625-5629.

Research output: Contribution to journalArticle

Harvard

Reith, AD, Bamborough, P, Jandu, K, Andreotti, D, Mensah, L, Dossang, P, Choi, HG, Deng, X, Zhang, J, Alessi, DR & Gray, NS 2012, 'GSK2578215A: a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor' Bioorganic & Medicinal Chemistry Letters, vol 22, no. 17, pp. 5625-5629.

APA

Reith, A. D., Bamborough, P., Jandu, K., Andreotti, D., Mensah, L., Dossang, P., Choi, H. G., Deng, X., Zhang, J., Alessi, D. R., & Gray, N. S. (2012). GSK2578215A: a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters, 22(17), 5625-5629doi: 10.1016/j.bmcl.2012.06.104

Vancouver

Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P et al. GSK2578215A: a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 2012;22(17):5625-5629.

Author

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

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 17, 2012, p. 5625-5629.

Research output: Contribution to journalArticle

Bibtex - Download

@article{82b1d2d5b8ea46cb91f9519ec91b38fb,
title = "GSK2578215A",
author = "Reith, {Alastair D.} and Paul Bamborough and Karamjit Jandu and Daniele Andreotti and Lucy Mensah and Pamela Dossang and Choi, {Hwan Geun} and Xianming Deng and Jinwei Zhang and Alessi, {Dario R.} and Gray, {Nathanael S.}",
year = "2012",
volume = "22",
number = "17",
pages = "5625--5629",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - GSK2578215A

T2 - a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

A1 - Reith,Alastair D.

A1 - Bamborough,Paul

A1 - Jandu,Karamjit

A1 - Andreotti,Daniele

A1 - Mensah,Lucy

A1 - Dossang,Pamela

A1 - Choi,Hwan Geun

A1 - Deng,Xianming

A1 - Zhang,Jinwei

A1 - Alessi,Dario R.

A1 - Gray,Nathanael S.

AU - Reith,Alastair D.

AU - Bamborough,Paul

AU - Jandu,Karamjit

AU - Andreotti,Daniele

AU - Mensah,Lucy

AU - Dossang,Pamela

AU - Choi,Hwan Geun

AU - Deng,Xianming

AU - Zhang,Jinwei

AU - Alessi,Dario R.

AU - Gray,Nathanael S.

PY - 2012

Y1 - 2012

N2 - 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 s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3-1.0 µM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg. © 2012 Elsevier Ltd. All rights reserved.

AB - 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 s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3-1.0 µM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg. © 2012 Elsevier Ltd. All rights reserved.

UR - http://www.scopus.com/inward/record.url?partnerID=yv4JPVwI&eid=2-s2.0-84864401977&md5=f9bfcb42ed8b7f832def295aeeef1e6d

U2 - 10.1016/j.bmcl.2012.06.104

DO - 10.1016/j.bmcl.2012.06.104

M1 - Article

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 17

VL - 22

SP - 5625

EP - 5629

ER -

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