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Page 1
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.
Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M. Vasbinder MM, et al. Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12. Bioorg Med Chem Lett. 2016. PMID: 26614408
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M. Grimster NP, et al. J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13. J Med Chem. 2018. PMID: 29856615
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M. Vasbinder MM, et al. J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23398453
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor.
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui CE, Deng N, Ferguson AD, Kawatkar S, Grimster NP, Ruston L, Lyne PD, Read JA, Peng X, Pei X, Fawell S, Tang Z, Throner S, Vasbinder MM, Wang H, Winter-Holt J, Woessner R, Wu A, Yang W, Zinda M, Kettle JG. Su Q, et al. Among authors: vasbinder mm. J Med Chem. 2020 May 14;63(9):4517-4527. doi: 10.1021/acs.jmedchem.9b01392. Epub 2020 Apr 28. J Med Chem. 2020. PMID: 32297743
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J. Oza V, et al. J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. J Med Chem. 2012. PMID: 22551018
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD. Janetka JW, et al. Among authors: vasbinder mm. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4242-8. doi: 10.1016/j.bmcl.2008.05.016. Epub 2008 May 6. Bioorg Med Chem Lett. 2008. PMID: 18547806
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D, Glossop S, Grebe T, Gu C, Hande S, Hawkins J, Hird AW, Holmes J, Horstick J, Jiang Y, Lamb ML, McGuire TM, Moore JE, O'Connell N, Pike A, Pike KG, Proia T, Roberts B, San Martin M, Sarkar U, Shao W, Stead D, Sumner N, Thakur K, Vasbinder MM, Varnes JG, Wang J, Wang L, Wu D, Wu L, Yang B, Yao T. Barlaam B, et al. Among authors: vasbinder mm. J Med Chem. 2020 Dec 24;63(24):15564-15590. doi: 10.1021/acs.jmedchem.0c01754. Epub 2020 Dec 11. J Med Chem. 2020. PMID: 33306391
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Barlaam B, De Savi C, Dishington A, Drew L, Ferguson AD, Ferguson D, Gu C, Hande S, Hassall L, Hawkins J, Hird AW, Holmes J, Lamb ML, Lister AS, McGuire TM, Moore JE, O'Connell N, Patel A, Pike KG, Sarkar U, Shao W, Stead D, Varnes JG, Vasbinder MM, Wang L, Wu L, Xue L, Yang B, Yao T. Barlaam B, et al. Among authors: vasbinder mm. J Med Chem. 2021 Oct 28;64(20):15189-15213. doi: 10.1021/acs.jmedchem.1c01249. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34647738
24 results