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Page 1
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.
Deng H, Zhou J, Sundersingh FS, Summerfield J, Somers D, Messer JA, Satz AL, Ancellin N, Arico-Muendel CC, Sargent Bedard KL, Beljean A, Belyanskaya SL, Bingham R, Smith SE, Boursier E, Carter P, Centrella PA, Clark MA, Chung CW, Davie CP, Delorey JL, Ding Y, Franklin GJ, Grady LC, Herry K, Hobbs C, Kollmann CS, Morgan BA, Pothier Kaushansky LJ, Zhou Q. Deng H, et al. Among authors: smith se. ACS Med Chem Lett. 2015 Jul 21;6(8):919-24. doi: 10.1021/acsmedchemlett.5b00179. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288694 Free PMC article.
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Bertrand SM, Ancellin N, Beaufils B, Bingham RP, Borthwick JA, Boullay AB, Boursier E, Carter PS, Chung CW, Churcher I, Dodic N, Fouchet MH, Fournier C, Francis PL, Gummer LA, Herry K, Hobbs A, Hobbs CI, Homes P, Jamieson C, Nicodeme E, Pickett SD, Reid IH, Simpson GL, Sloan LA, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Valko K, Washio Y, Young RJ. Bertrand SM, et al. Among authors: smith se. J Med Chem. 2015 Sep 24;58(18):7140-63. doi: 10.1021/acs.jmedchem.5b00313. Epub 2015 Jul 2. J Med Chem. 2015. PMID: 26090771
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Borthwick JA, Ancellin N, Bertrand SM, Bingham RP, Carter PS, Chung CW, Churcher I, Dodic N, Fournier C, Francis PL, Hobbs A, Jamieson C, Pickett SD, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Young RJ. Borthwick JA, et al. Among authors: smith se. J Med Chem. 2016 Mar 24;59(6):2452-67. doi: 10.1021/acs.jmedchem.5b01607. Epub 2016 Mar 16. J Med Chem. 2016. PMID: 26938474 Free article.
Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors.
Deng H, Zhou J, Sundersingh F, Messer JA, Somers DO, Ajakane M, Arico-Muendel CC, Beljean A, Belyanskaya SL, Bingham R, Blazensky E, Boullay AB, Boursier E, Chai J, Carter P, Chung CW, Daugan A, Ding Y, Herry K, Hobbs C, Humphries E, Kollmann C, Nguyen VL, Nicodeme E, Smith SE, Dodic N, Ancellin N. Deng H, et al. Among authors: smith se. ACS Med Chem Lett. 2016 Feb 8;7(4):379-84. doi: 10.1021/acsmedchemlett.5b00389. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096045 Free PMC article.
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN. Down K, et al. Among authors: smith s. J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3. J Med Chem. 2015. PMID: 26301626
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Walker MC, Schweitzer BA, Madsen HM, Tenbrink RE, McDonald J, Smith SE, Foltin S, Beidler D, Thorarensen A. Meyers MJ, et al. Among authors: smith se. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6538-44. doi: 10.1016/j.bmcl.2011.08.055. Epub 2011 Aug 22. Bioorg Med Chem Lett. 2011. PMID: 21924614
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Schweitzer BA, Wilcox MV, McDonald J, Smith SE, Foltin S, Rumsey J, Yang YS, Walker MC, Kamtekar S, Beidler D, Thorarensen A. Meyers MJ, et al. Among authors: smith se. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6545-53. doi: 10.1016/j.bmcl.2011.08.048. Epub 2011 Aug 19. Bioorg Med Chem Lett. 2011. PMID: 21924613
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).
Johnson DS, Ahn K, Kesten S, Lazerwith SE, Song Y, Morris M, Fay L, Gregory T, Stiff C, Dunbar JB Jr, Liimatta M, Beidler D, Smith S, Nomanbhoy TK, Cravatt BF. Johnson DS, et al. Among authors: smith s. Bioorg Med Chem Lett. 2009 May 15;19(10):2865-9. doi: 10.1016/j.bmcl.2009.03.080. Epub 2009 Mar 24. Bioorg Med Chem Lett. 2009. PMID: 19386497 Free PMC article.
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.
Young RJ, Beams RM, Carter K, Clark HA, Coe DM, Chambers CL, Davies PI, Dawson J, Drysdale MJ, Franzman KW, French C, Hodgson ST, Hodson HF, Kleanthous S, Rider P, Sanders D, Sawyer DA, Scott KJ, Shearer BG, Stocker R, Smith S, Tackley MC, Knowles RG. Young RJ, et al. Bioorg Med Chem Lett. 2000 Mar 20;10(6):597-600. doi: 10.1016/s0960-894x(00)00055-x. Bioorg Med Chem Lett. 2000. PMID: 10741561
1,030 results