Year |
Citation |
Score |
2020 |
Su Q, Banks E, Bebernitz G, Bell K, Borenstein CF, Chen H, Chuaqui C, Deng N, Ferguson AD, Kawatkar SP, Grimster NP, Ruston L, Lyne P, Read JA, Peng XY, et al. 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 (JAK1) inhibitor. Journal of Medicinal Chemistry. PMID 32297743 DOI: 10.1021/Acs.Jmedchem.9B01392 |
0.411 |
|
2019 |
Hu S, Marineau J, Hamman K, Bradley M, Savinainen A, Alnemy S, Rajagopal N, Orlando D, Chuaqui C, Olson E. Abstract 4421: SY-5609, an orally available selective CDK7 inhibitor demonstrates broad anti-tumor activity in vivo Cancer Research. 79: 4421-4421. DOI: 10.1158/1538-7445.Sabcs18-4421 |
0.346 |
|
2018 |
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 PD, Read JA, et al. Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors. Journal of Medicinal Chemistry. PMID 29856615 DOI: 10.1021/Acs.Jmedchem.8B00076 |
0.428 |
|
2017 |
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, et al. Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors. Journal of Medicinal Chemistry. PMID 28485934 DOI: 10.1021/Acs.Jmedchem.7B00359 |
0.389 |
|
2017 |
Kettle JG, Su Q, Grimster N, Kawatkar S, Throner S, Woessner R, Chen H, Bebernitz G, Bell K, Anderson E, Ruston L, Winter-Holt J, Lyne P, Vasbinder M, Chuaqui C. Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205 Cancer Research. 77: 979-979. DOI: 10.1158/1538-7445.Am2017-979 |
0.422 |
|
2016 |
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. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. Acs Medicinal Chemistry Letters. 7: 1118-1123. PMID 27994749 DOI: 10.1021/Acsmedchemlett.6B00322 |
0.428 |
|
2016 |
Akçay G, Belmonte MA, Aquila B, Chuaqui C, Hird AW, Lamb ML, Rawlins PB, Su N, Tentarelli S, Grimster NP, Su Q. Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain. Nature Chemical Biology. PMID 27595327 DOI: 10.1038/Nchembio.2174 |
0.341 |
|
2016 |
Hennessy EJ, Chuaqui C, Ashton S, Colclough N, Cross DA, Debreczeni JÉ, Eberlein C, Gingipalli L, Klinowska TC, Orme JP, Sha L, Wu X. Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation. Acs Medicinal Chemistry Letters. 7: 514-519. PMID 27190603 DOI: 10.1021/Acsmedchemlett.6B00058 |
0.372 |
|
2016 |
Dowling JE, Alimzhanov M, Bao L, Chuaqui C, Denz CR, Jenkins E, Larsen NA, Lyne PD, Pontz T, Ye Q, Holdgate GA, Snow L, O'Connell N, Ferguson AD. Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo. Acs Medicinal Chemistry Letters. 7: 300-5. PMID 26985319 DOI: 10.1021/Acsmedchemlett.5B00452 |
0.361 |
|
2015 |
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, et al. Identification of azabenzimidazoles as potent JAK1 selective inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 26614408 DOI: 10.1016/J.Bmcl.2015.11.031 |
0.376 |
|
2014 |
Yang B, Lamb ML, Zhang T, Hennessy EJ, Grewal G, Sha L, Zambrowski M, Block MH, Dowling JE, Su N, Wu J, Deegan T, Mikule K, Wang W, Kaspera R, ... Chuaqui C, et al. Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening. Journal of Medicinal Chemistry. 57: 9958-70. PMID 25458601 DOI: 10.1021/Jm501179R |
0.392 |
|
2014 |
Johannes JW, Chuaqui C, Cowen S, Devereaux E, Gingipalli L, Molina A, Wang T, Whitston D, Wu X, Zhang HJ, Zinda M. Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases. Bioorganic & Medicinal Chemistry Letters. 24: 1138-43. PMID 24462666 DOI: 10.1016/J.Bmcl.2013.12.123 |
0.433 |
|
2014 |
Su Q, Ioannidis S, Chuaqui C, Almeida L, Alimzhanov M, Bebernitz G, Bell K, Block M, Howard T, Huang S, Huszar D, Read JA, Rivard Costa C, Shi J, Su M, et al. Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. Journal of Medicinal Chemistry. 57: 144-58. PMID 24359159 DOI: 10.1021/Jm401546N |
0.377 |
|
2014 |
McCoull W, Hennessy EJ, Blades K, Box MR, Chuaqui C, Dowling JE, Davies CD, Ferguson AD, Goldberg FW, Howe NJ, Kemmitt PD, Lamont GM, Madden K, McWhirter C, Varnes JG, et al. Identification and optimisation of 7-azaindole PAK1 inhibitors with improved potency and kinase selectivity Medchemcomm. 5: 1533-1539. DOI: 10.1039/C4Md00280F |
0.43 |
|
2013 |
Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA, Peng B, Pontz TW, Rivard-Costa C, Saeh JC, Thakur K, et al. Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. Acs Medicinal Chemistry Letters. 4: 800-5. PMID 24900749 DOI: 10.1021/Ml400197U |
0.388 |
|
2013 |
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, et al. Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). Journal of Medicinal Chemistry. 56: 7025-48. PMID 23930994 DOI: 10.1021/Jm400822Z |
0.387 |
|
2013 |
Wu J, Mikule K, Wang W, Su N, Petteruti P, Gharahdaghi F, Code E, Zhu X, Jacques K, Lai Z, Yang B, Lamb ML, Chuaqui C, Keen N, Chen H. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. Acs Chemical Biology. 8: 2201-8. PMID 23895133 DOI: 10.1021/Cb400186W |
0.303 |
|
2013 |
Woessner R, Bebernitz G, Bell K, Caccese R, Johnson N, Kettle J, Rivard C, Schroeder P, Su Q, Wang H, Ye M, Zheng W, Zinda M, Lyne P, Vasbinder M, ... ... Chuaqui C, et al. Abstract 931: Highly selective JAK1 kinase inhibitors suppress Y705-mediated STAT3 activation in a wide range of tumor types, with reduced hematological toxicity. Cancer Research. 73: 931-931. DOI: 10.1158/1538-7445.Am2013-931 |
0.384 |
|
2013 |
Lamb ML, Wu J, Mikule K, Wang W, Su N, Petteruti P, Gharahdaghi F, Code E, Zhu X, Jacques K, Lai Z, Zhang T, Boulay D, Grewal G, Keen N, ... ... Chuaqui C, et al. Abstract C55: Discovery and optimization of inhibitors of the KIFC1 motor protein. Molecular Cancer Therapeutics. 12. DOI: 10.1158/1535-7163.Targ-13-C55 |
0.334 |
|
2013 |
Finlay MRV, Anderton M, Ashton S, Ballard PG, Bradbury RH, Butterworth S, Chuaqui CE, Colclough N, Cross DAE, McFarland HL, Mellor MJ, Ward RA, Waring MJ. Abstract B94: Discovery of and first disclosure of the clinical candidate AZD9291, a potent and selective third-generation EGFR inhibitor of both activating and T790M resistant mutations that spares the wild type form of the receptor. Molecular Cancer Therapeutics. 12. DOI: 10.1158/1535-7163.Targ-13-B94 |
0.366 |
|
2012 |
Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D, Pollard H, Lee JW, Peng B, Thakur K, Ye Q, et al. Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. Acs Medicinal Chemistry Letters. 3: 278-83. PMID 24900464 DOI: 10.1021/Ml200257N |
0.427 |
|
2012 |
Wang T, Block MA, Cowen S, Davies AM, Devereaux E, Gingipalli L, Johannes J, Larsen NA, Su Q, Tucker JA, Whitston D, Wu J, Zhang HJ, Zinda M, Chuaqui C. Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases. Bioorganic & Medicinal Chemistry Letters. 22: 2063-9. PMID 22305584 DOI: 10.1016/J.Bmcl.2012.01.018 |
0.405 |
|
2010 |
Guckian K, Carter MB, Lin EY, Choi M, Sun L, Boriack-Sjodin PA, Chuaqui C, Lane B, Cheung K, Ling L, Lee WC. Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 20: 326-9. PMID 19914068 DOI: 10.1016/J.Bmcl.2009.10.108 |
0.376 |
|
2009 |
Nandigam RK, Kim S, Singh J, Chuaqui C. Position specific interaction dependent scoring technique for virtual screening based on weighted protein--ligand interaction fingerprint profiles. Journal of Chemical Information and Modeling. 49: 1185-92. PMID 19415918 DOI: 10.1021/Ci800466N |
0.301 |
|
2009 |
Bonafoux D, Chuaqui C, Boriack-Sjodin PA, Fitch C, Hankins G, Josiah S, Black C, Hetu G, Ling L, Lee W. 2-Aminoimidazoles inhibitors of TGF-beta receptor 1. Bioorganic & Medicinal Chemistry Letters. 19: 912-916. PMID 19135364 DOI: 10.1016/J.Bmcl.2008.11.119 |
0.311 |
|
2008 |
Fu K, Corbley MJ, Sun L, Friedman JE, Shan F, Papadatos JL, Costa D, Lutterodt F, Sweigard H, Bowes S, Choi M, Boriack-Sjodin PA, Arduini RM, Sun D, Newman MN, ... ... Chuaqui CE, et al. SM16, an orally active TGF-beta type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model. Arteriosclerosis, Thrombosis, and Vascular Biology. 28: 665-71. PMID 18202322 DOI: 10.1161/Atvbaha.107.158030 |
0.322 |
|
2006 |
Sun D, Chuaqui C, Deng Z, Bowes S, Chin D, Singh J, Cullen P, Hankins G, Lee WC, Donnelly J, Friedman J, Josiah S. A kinase-focused compound collection: compilation and screening strategy. Chemical Biology & Drug Design. 67: 385-94. PMID 16882313 DOI: 10.1111/J.1747-0285.2006.00396.X |
0.382 |
|
2006 |
Singh J, Deng Z, Narale G, Chuaqui C. Structural Interaction Fingerprints: A New Approach to Organizing, Mining, Analyzing, and Designing Protein–Small Molecule Complexes Chemical Biology & Drug Design. 67: 5-12. PMID 16492144 DOI: 10.1111/J.1747-0285.2005.00323.X |
0.331 |
|
2006 |
Deng Z, Chuaqui C, Singh J. Knowledge-based design of target-focused libraries using protein-ligand interaction constraints. Journal of Medicinal Chemistry. 49: 490-500. PMID 16420036 DOI: 10.1021/Jm050381X |
0.342 |
|
2005 |
Chuaqui C, Deng Z, Singh J. Interaction Profiles of Protein Kinase−Inhibitor Complexes and Their Application to Virtual Screening Journal of Medicinal Chemistry. 48: 121-133. PMID 15634006 DOI: 10.1021/Jm049312T |
0.396 |
|
2004 |
Chin DN, Chuaqui CE, Singh J. Integration of virtual screening into the drug discovery process Mini-Reviews in Medicinal Chemistry. 4: 1053-1065. PMID 15579113 DOI: 10.2174/1389557043403044 |
0.32 |
|
2004 |
Singh J, Chuaqui C, Annboriacksjodin P, Lee W, Pontz T, Corbley M, Cheung H, Arduini R, Mead J, Newman M. Corrigendum to “Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI)”: [Bioorg. Med. Chem. Lett. 13 (2003) 4355] Bioorganic & Medicinal Chemistry Letters. 14: 2991. DOI: 10.1016/S0960-894X(04)00379-8 |
0.38 |
|
2004 |
Singh J, Chuaqui CE, Boriack-Sjodin PA, Lee W, Pontz T, Corbley MJ, Cheung H-, Arduini RM, Mead JN, Newman MN, Papadatos JL, Bowes S, Josiah S, Ling LE. Corrigendum to “Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI)” Bioorganic & Medicinal Chemistry Letters. 14: 2991. DOI: 10.1016/J.Bmcl.2004.03.027 |
0.358 |
|
2003 |
Singh J, Chuaqui CE, Boriack-Sjodin PA, Lee WC, Pontz T, Corbley MJ, Cheung HK, Arduini RM, Mead JN, Newman MN, Papadatos JL, Bowes S, Josiah S, Ling LE. Successful shape-Based virtual screening: The discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI) Bioorganic and Medicinal Chemistry Letters. 13: 4355-4359. PMID 14643325 DOI: 10.1016/J.Bmcl.2003.09.028 |
0.425 |
|
1996 |
Thachuk M, Chuaqui CE, Le Roy RJ. Linewidths and shifts of very low temperature CO in He: A challenge for theory or experiment? Journal of Chemical Physics. 105: 4005-4014. DOI: 10.1063/1.472274 |
0.546 |
|
1996 |
Bissonnette C, Chuaqui CE, Crowell KG, Le Roy RJ, Wheatley RJ, Meath WJ. A reliable new potential energy surface for H2-Ar Journal of Chemical Physics. 105: 2639-2653. DOI: 10.1063/1.472127 |
0.571 |
|
1994 |
Chuaqui CE, Le Roy RJ, McKellar ARW. Infrared spectrum and potential energy surface of He-CO The Journal of Chemical Physics. 101: 39-61. DOI: 10.1063/1.468147 |
0.581 |
|
1992 |
Slee T, Le Roy RJ, Chuaqui CE. Calculated rovibrational energy levels and infrared spectrum of he–c2h2 Molecular Physics. 77: 111-134. DOI: 10.1080/00268979200102341 |
0.564 |
|
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