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Page 1
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS. Cheung M, et al. Among authors: brooks ca. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523109 Free PMC article.
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Eidam HS, Fox RM, Hammond M, Hoang TH, Holt DA, Hilfiker MA, Lawhorn BG, Patterson JR, Stoy P, Roethke TJ, Ye G, Zhao S, Thorneloe KS, Goodman KB, Cheung M. Brooks CA, et al. ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. doi: 10.1021/acsmedchemlett.9b00274. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413810 Free PMC article.
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Brnardic EJ, Costell MH, Holt DA, Jolivette LJ, Matthews JM, McAtee JJ, McCleland BW, Patterson JR, Pero JE, Rivero RA, Roethke TJ, Sanchez RM, Shenje R, Terrell LR, Lawhorn BG. Brooks CA, et al. J Med Chem. 2019 Oct 24;62(20):9270-9280. doi: 10.1021/acs.jmedchem.9b01247. Epub 2019 Oct 9. J Med Chem. 2019. PMID: 31532662
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
Jin J, Morales-Ramos A, Eidam P, Mecom J, Li Y, Brooks C, Hilfiker M, Zhang D, Wang N, Shi D, Tseng PS, Wheless K, Budzik B, Evans K, Jaworski JP, Jugus J, Leon L, Wu C, Pullen M, Karamshi B, Rao P, Ward E, Laping N, Evans C, Leach C, Holt D, Su X, Morrow D, Fries H, Thorneloe K, Edwards R. Jin J, et al. ACS Med Chem Lett. 2010 May 14;1(7):316-20. doi: 10.1021/ml100077x. eCollection 2010 Oct 14. ACS Med Chem Lett. 2010. PMID: 24900213 Free PMC article.
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG. Brnardic EJ, et al. J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18. J Med Chem. 2018. PMID: 30335378
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG. Pero JE, et al. Among authors: brooks c. J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30500190
Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.
Morales-Ramos ÁI, Li YH, Hilfiker M, Mecom JS, Eidam P, Shi D, Tseng PS, Brooks C, Zhang D, Wang N, Jaworski JP, Morrow D, Fries H, Edwards R, Jin J. Morales-Ramos ÁI, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2806-11. doi: 10.1016/j.bmcl.2011.03.107. Epub 2011 Apr 5. Bioorg Med Chem Lett. 2011. PMID: 21514150
In vivo activity of an azole series of CCR2 antagonists.
Smethurst CA, Bevan N, Brooks C, Emmons A, Gough PJ, Mookherjee C, Moores K, Peace S, Philp J, Piercy V, Watson SP, Zippoli M. Smethurst CA, et al. Among authors: brooks c. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7252-5. doi: 10.1016/j.bmcl.2012.09.020. Epub 2012 Sep 23. Bioorg Med Chem Lett. 2012. PMID: 23079519
Identification of a sulfonamide series of CCR2 antagonists.
Peace S, Philp J, Brooks C, Piercy V, Moores K, Smethurst C, Watson S, Gaines S, Zippoli M, Mookherjee C, Ife R. Peace S, et al. Bioorg Med Chem Lett. 2010 Jul 1;20(13):3961-4. doi: 10.1016/j.bmcl.2010.04.142. Epub 2010 May 7. Bioorg Med Chem Lett. 2010. PMID: 20627722
70 results