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Page 1
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
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, Zhang T, Brassil P, Racicot V, Bao L, Denz CR, Cooke E. Dowling JE, et al. Among authors: thakur k. ACS Med Chem Lett. 2012 Jan 24;3(4):278-83. doi: 10.1021/ml200257n. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900464 Free PMC article.
3-amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor.
Scott DA, Dakin LA, Del Valle DJ, Diebold RB, Drew L, Gero TW, Ogoe CA, Omer CA, Repik G, Thakur K, Ye Q, Zheng X. Scott DA, et al. Among authors: thakur k. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1382-4. doi: 10.1016/j.bmcl.2011.01.033. Epub 2011 Jan 14. Bioorg Med Chem Lett. 2011. PMID: 21295474
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
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, Ye Q, Zhang T, Lyne PD. Dowling JE, et al. Among authors: thakur k. ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. doi: 10.1021/ml400197u. eCollection 2013 Aug 8. ACS Med Chem Lett. 2013. PMID: 24900749 Free PMC article.
Target Deconvolution Efforts on Wnt Pathway Screen Reveal Dual Modulation of Oxidative Phosphorylation and SERCA2.
Casás-Selves M, Zhang AX, Dowling JE, Hallén S, Kawatkar A, Pace NJ, Denz CR, Pontz T, Garahdaghi F, Cao Q, Sabirsh A, Thakur K, O'Connell N, Hu J, Cornella-Taracido I, Weerapana E, Zinda M, Goodnow RA Jr, Castaldi MP. Casás-Selves M, et al. Among authors: thakur k. ChemMedChem. 2017 Jun 21;12(12):917-924. doi: 10.1002/cmdc.201700028. Epub 2017 Apr 26. ChemMedChem. 2017. PMID: 28371485
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. Among authors: thakur k. 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
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: thakur k. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.
Chen JJ, Thakur KD, Clark MP, Laughlin SK, George KM, Bookland RG, Davis JR, Cabrera EJ, Easwaran V, De B, George Zhang Y. Chen JJ, et al. Among authors: thakur kd. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5633-8. doi: 10.1016/j.bmcl.2006.08.022. Epub 2006 Aug 24. Bioorg Med Chem Lett. 2006. PMID: 16934457
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: thakur k. 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
718 results