Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase-Reference-Cited by-同舟云学术

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase

Published:2019-04-23 Issue:10 Volume:62 Page:5096-5110
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Harris Philip A.^ORCID,Faucher Nicolas¹,George Nicolas¹,Eidam Patrick M.,King Bryan W.,White Gemma V.²,Anderson Niall A.²^ORCID,Bandyopadhyay Deepak,Beal Allison M.,Beneton Veronique¹,Berger Scott B.,Campobasso Nino,Campos Sebastien²,Capriotti Carol A.,Cox Julie A.,Daugan Alain¹,Donche Frederic¹,Fouchet Marie-Hélène¹,Finger Joshua N.,Geddes Brad,Gough Peter J.,Grondin Pascal¹,Hoffman Bonnie L.,Hoffman Sandra J.,Hutchinson Susan E.²,Jeong Jae U.,Jigorel Emilie¹,Lamoureux Pauline¹,Leister Lara K.,Lich John D.,Mahajan Mukesh K.,Meslamani Jamel^ORCID,Mosley Julie E.²,Nagilla Rakesh,Nassau Pamela M.²,Ng Sze-Ling,Ouellette Michael T.,Pasikanti Kishore K.,Potvain Florent¹,Reilly Michael A.,Rivera Elizabeth J.,Sautet Stéphane¹,Schaeffer Michelle C.,Sehon Clark A.,Sun Helen,Thorpe James H.²,Totoritis Rachel D.,Ward Paris,Wellaway Natalie²,Wisnoski David D.,Woolven James M.²,Bertin John,Marquis Robert W.

Affiliation:

1. Flexible Discovery Unit, GlaxoSmithKline, 25-27 avenue du Québec, 91951 Les Ulis Cedex, France

2. Flexible Discovery Unit, GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b00318

Reference24 articles.

1. Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice

2. RIPK1 ensures intestinal homeostasis by protecting the epithelium against apoptosis