Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

22 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
Page 1
Structure-Based Design of Selective Noncovalent CDK12 Inhibitors.
Johannes JW, Denz CR, Su N, Wu A, Impastato AC, Mlynarski S, Varnes JG, Prince DB, Cidado J, Gao N, Haddrick M, Jones NH, Li S, Li X, Liu Y, Nguyen TB, O'Connell N, Rivers E, Robbins DW, Tomlinson R, Yao T, Zhu X, Ferguson AD, Lamb ML, Manchester JI, Guichard S. Johannes JW, et al. Among authors: varnes jg. ChemMedChem. 2018 Feb 6;13(3):231-235. doi: 10.1002/cmdc.201700695. Epub 2018 Jan 26. ChemMedChem. 2018. PMID: 29266803
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: varnes jg. 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
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: varnes jg. 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 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: varnes jg. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.
McCoull W, Hennessy EJ, Blades K, Chuaqui C, Dowling JE, Ferguson AD, Goldberg FW, Howe N, Jones CR, Kemmitt PD, Lamont G, Varnes JG, Ward RA, Yang B. McCoull W, et al. Among authors: varnes jg. ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. doi: 10.1021/acsmedchemlett.6b00322. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994749 Free PMC article.
AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia.
Balachander SB, Criscione SW, Byth KF, Cidado J, Adam A, Lewis P, Macintyre T, Wen S, Lawson D, Burke K, Lubinski T, Tyner JW, Kurtz SE, McWeeney SK, Varnes J, Diebold RB, Gero T, Ioannidis S, Hennessy EJ, McCoull W, Saeh JC, Tabatabai A, Tavana O, Su N, Schuller A, Garnett MJ, Jaaks P, Coker EA, Gregory GP, Newbold A, Johnstone RW, Gangl E, Wild M, Zinda M, Secrist JP, Davies BR, Fawell SE, Gibbons FD. Balachander SB, et al. Clin Cancer Res. 2020 Dec 15;26(24):6535-6549. doi: 10.1158/1078-0432.CCR-20-0863. Epub 2020 Sep 28. Clin Cancer Res. 2020. PMID: 32988967
Towards the next generation of dual Bcl-2/Bcl-xL inhibitors.
Varnes JG, Gero T, Huang S, Diebold RB, Ogoe C, Grover PT, Su M, Mukherjee P, Saeh JC, MacIntyre T, Repik G, Dillman K, Byth K, Russell DJ, Ioannidis S. Varnes JG, et al. Bioorg Med Chem Lett. 2014 Jul 15;24(14):3026-33. doi: 10.1016/j.bmcl.2014.05.036. Epub 2014 May 20. Bioorg Med Chem Lett. 2014. PMID: 24881567
Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.
Varnes JG, Xiong H, Forst JM, Holmquist CR, Ernst GE, Frietze W, Dembofsky B, Andisik DW, Palmer WE, Hinkley L, Steelman GB, Wilkins DE, Tian G, Jonak G, Potts WM, Wang X, Brugel TA, Alhambra C, Wood MW, Veale CA, Albert JS. Varnes JG, et al. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1043-1049. doi: 10.1016/j.bmcl.2018.02.029. Epub 2018 Feb 14. Bioorg Med Chem Lett. 2018. PMID: 29486970
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Scott JS, Moss TA, Balazs A, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Davey PRJ, Delpuech O, Fawell S, Fisher DI, Gagrica S, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Herlihy K, Hughes S, Hunt TA, Huynh H, Janbon SLM, Johnson T, Kavanagh S, Klinowska T, Lawson M, Lister AS, Marden S, McGinnity DF, Morrow CJ, Nissink JWM, O'Donovan DH, Peng B, Polanski R, Stead DS, Stokes S, Thakur K, Throner SR, Tucker MJ, Varnes J, Wang H, Wilson DM, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. J Med Chem. 2020 Dec 10;63(23):14530-14559. doi: 10.1021/acs.jmedchem.0c01163. Epub 2020 Sep 29. J Med Chem. 2020. PMID: 32910656
22 results