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Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Yang MG, et al. Among authors: chen j. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891130 Free PMC article.
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC. Carter PH, et al. Among authors: chen j. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25893046 Free PMC article.
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate.
Cherney RJ, Anjanappa P, Selvakumar K, Batt DG, Brown GD, Rose AV, Vuppugalla R, Chen J, Pang J, Xu S, Yarde M, Tebben AJ, Paidi VR, Cvijic ME, Mathur A, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Cherney RJ, et al. Among authors: chen j. ACS Med Chem Lett. 2021 Oct 15;12(11):1753-1758. doi: 10.1021/acsmedchemlett.1c00373. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795864 Free PMC article.
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Shan W, Balog A, Nation A, Zhu X, Chen J, Cvijic ME, Geng J, Rizzo CA, Spires T Jr, Attar RM, Obermeier M, Traeger S, Dai J, Zhang Y, Galella M, Trainor G, Vite GD, Gavai AV. Shan W, et al. Among authors: chen j. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5707-5711. doi: 10.1016/j.bmcl.2016.10.059. Epub 2016 Oct 21. Bioorg Med Chem Lett. 2016. PMID: 27836399
Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.
Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS. Liu C, et al. Among authors: chen j, chen c. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891145 Free PMC article.
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.
Xiao HY, Li N, Duan JJ, Jiang B, Lu Z, Ngu K, Tino J, Kopcho LM, Lu H, Chen J, Tebben AJ, Sheriff S, Chang CY, Yanchunas J Jr, Calambur D, Gao M, Shuster DJ, Susulic V, Xie JH, Guarino VR, Wu DR, Gregor KR, Goldstine CB, Hynes J Jr, Macor JE, Salter-Cid L, Burke JR, Shaw PJ, Dhar TGM. Xiao HY, et al. Among authors: chen j. J Med Chem. 2020 Dec 10;63(23):15050-15071. doi: 10.1021/acs.jmedchem.0c01732. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33261314
GPCR assay automation for leveraging lead optimization.
Cvijic ME, Chen J, Kubala S, Nolfo J, Kolodin G, Zhang L. Cvijic ME, et al. Among authors: chen j. J Lab Autom. 2012 Aug;17(4):266-74. doi: 10.1177/2211068212442502. Epub 2012 Apr 13. J Lab Autom. 2012. PMID: 22505604
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