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Page 1
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: leblanc c. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J, Schadt HS, Couttet P, Wolf A, Wang Y, Barzaghi-Rinaudo P, Murakami M, Kauffmann A, Knoepfel T, Buschmann N, Leblanc C, Mah R, Furet P, Blank J, Hofmann F, Sellers WR, Graus Porta D. Weiss A, et al. Among authors: leblanc c. Mol Cancer Ther. 2019 Dec;18(12):2194-2206. doi: 10.1158/1535-7163.MCT-18-1291. Epub 2019 Aug 13. Mol Cancer Ther. 2019. PMID: 31409633
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: leblanc c. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
Sandham DA, Arnold N, Aschauer H, Bala K, Barker L, Brown L, Brown Z, Budd D, Cox B, Docx C, Dubois G, Duggan N, England K, Everatt B, Furegati M, Hall E, Kalthoff F, King A, Leblanc CJ, Manini J, Meingassner J, Profit R, Schmidt A, Simmons J, Sohal B, Stringer R, Thomas M, Turner KL, Walker C, Watson SJ, Westwick J, Willis J, Williams G, Wilson C. Sandham DA, et al. Among authors: leblanc cj. Bioorg Med Chem. 2013 Nov 1;21(21):6582-91. doi: 10.1016/j.bmc.2013.08.025. Epub 2013 Aug 22. Bioorg Med Chem. 2013. PMID: 24021582
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Sandham DA, Adcock C, Bala K, Barker L, Brown Z, Dubois G, Budd D, Cox B, Fairhurst RA, Furegati M, Leblanc C, Manini J, Profit R, Reilly J, Stringer R, Schmidt A, Turner KL, Watson SJ, Willis J, Williams G, Wilson C. Sandham DA, et al. Among authors: leblanc c. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042. Epub 2009 Jun 14. Bioorg Med Chem Lett. 2009. PMID: 19592244
Correction to "Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma".
Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Leblanc C, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J. Sandham DA, et al. Among authors: leblanc c. ACS Med Chem Lett. 2017 Sep 1;8(9):987. doi: 10.1021/acsmedchemlett.7b00353. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947949 Free PMC article.
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
Sandham DA, Aldcroft C, Baettig U, Barker L, Beer D, Bhalay G, Brown Z, Dubois G, Budd D, Bidlake L, Campbell E, Cox B, Everatt B, Harrison D, Leblanc CJ, Manini J, Profit R, Stringer R, Thompson KS, Turner KL, Tweed MF, Walker C, Watson SJ, Whitebread S, Willis J, Williams G, Wilson C. Sandham DA, et al. Among authors: leblanc cj. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. doi: 10.1016/j.bmcl.2007.05.019. Epub 2007 May 13. Bioorg Med Chem Lett. 2007. PMID: 17531480
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Bruce I, Akhlaq M, Bloomfield GC, Budd E, Cox B, Cuenoud B, Finan P, Gedeck P, Hatto J, Hayler JF, Head D, Keller T, Kirman L, Leblanc C, Le Grand D, McCarthy C, O'Connor D, Owen C, Oza MS, Pilgrim G, Press NE, Sviridenko L, Whitehead L. Bruce I, et al. Among authors: leblanc c. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5445-50. doi: 10.1016/j.bmcl.2012.07.042. Epub 2012 Jul 17. Bioorg Med Chem Lett. 2012. PMID: 22863202
Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P. Fairhurst RA, et al. Among authors: leblanc c. Medchemcomm. 2017 Jun 8;8(8):1604-1613. doi: 10.1039/c7md00213k. eCollection 2017 Aug 1. Medchemcomm. 2017. PMID: 30108871 Free PMC article.
470 results