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Items: 23

1.

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.

Burke JR, Cheng L, Gillooly KM, Strnad J, Zupa-Fernandez A, Catlett IM, Zhang Y, Heimrich EM, McIntyre KW, Cunningham MD, Carman JA, Zhou X, Banas D, Chaudhry C, Li S, D'Arienzo C, Chimalakonda A, Yang X, Xie JH, Pang J, Zhao Q, Rose SM, Huang J, Moslin RM, Wrobleski ST, Weinstein DS, Salter-Cid LM.

Sci Transl Med. 2019 Jul 24;11(502). pii: eaaw1736. doi: 10.1126/scitranslmed.aaw1736.

PMID:
31341059
2.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.

J Med Chem. 2019 Jul 18. doi: 10.1021/acs.jmedchem.9b00444. [Epub ahead of print]

PMID:
31318208
3.

Pharmacokinetics of 40‚ÄČkDa PEG in rodents using high-field NMR spectroscopy.

Khandelwal P, Zhang L, Chimalakonda A, Caceres-Cortes J, Huang C, Marathe P, Reily MD.

J Pharm Biomed Anal. 2019 Jul 15;171:30-34. doi: 10.1016/j.jpba.2019.03.066. Epub 2019 Apr 1.

PMID:
30959317
4.

Preclinical QSP Modeling in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape.

Nijsen MJMA, Wu F, Bansal L, Bradshaw-Pierce E, Chan JR, Liederer BM, Mettetal JT, Schroeder P, Schuck E, Tsai A, Xu C, Chimalakonda A, Le K, Penney M, Topp B, Yamada A, Spilker ME.

CPT Pharmacometrics Syst Pharmacol. 2018 Mar;7(3):135-146. doi: 10.1002/psp4.12282. Epub 2018 Feb 1. Review.

5.

Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide.

Gunaga P, Lloyd J, Mummadi S, Banerjee A, Dhondi NK, Hennan J, Subray V, Jayaram R, Rajugowda N, Umamaheshwar Reddy K, Kumaraguru D, Mandal U, Beldona D, Adisechen AK, Yadav N, Warrier J, Johnson JA, Sale H, Putlur SP, Saxena A, Chimalakonda A, Mandlekar S, Conder M, Xing D, Gupta AK, Gupta A, Rampulla R, Mathur A, Levesque P, Wexler RR, Finlay HJ.

J Med Chem. 2017 May 11;60(9):3795-3803. doi: 10.1021/acs.jmedchem.6b01889. Epub 2017 Apr 28.

PMID:
28418664
6.

Antibody Drug-Target Engagement Measurement in Tissue Using Quantitative Affinity Extraction Liquid Chromatography-Mass Spectrometry: Method Development and Qualification.

Ciccimaro E, Zhu Y, Ostanin D, Suchard S, MacGuire J, Xiao Q, Dongre A, Chimalakonda A, Olah T, Shipkova P.

Anal Chem. 2017 May 2;89(9):5115-5123. doi: 10.1021/acs.analchem.7b00688. Epub 2017 Apr 21.

PMID:
28383906
7.

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.

Finlay HJ, Johnson JA, Lloyd JL, Jiang J, Neels J, Gunaga P, Banerjee A, Dhondi N, Chimalakonda A, Mandlekar S, Conder ML, Sale H, Xing D, Levesque P, Wexler RR.

ACS Med Chem Lett. 2016 Jun 9;7(9):831-4. doi: 10.1021/acsmedchemlett.6b00117. eCollection 2016 Sep 8.

8.

LC-MS/MS multiplexed assay for the quantitation of a therapeutic protein BMS-986089 and the target protein Myostatin.

Zhu Y, D'Arienzo C, Lou Z, Kozhich A, Madireddi M, Chimalakonda A, Tymiak A, Olah TV.

Bioanalysis. 2016 Feb;8(3):193-204. doi: 10.4155/bio.15.238. Epub 2016 Jan 26.

PMID:
26811930
9.

Pseudosaccharin amines as potent and selective KV1.5 blockers.

Lloyd J, Finlay HJ, Kover A, Johnson J, Pi Z, Jiang J, Neels J, Cavallaro C, Wexler R, Conder ML, Shi H, Li D, Sun H, Chimalakonda A, Huang C, Salvati M, Levesque P.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4983-4986. doi: 10.1016/j.bmcl.2015.02.066. Epub 2015 Mar 7.

PMID:
25801931
10.

Development and characterization of a free therapeutic ligand binding assay with assistance from kinetics modeling.

Williams L, Sank M, Chimalakonda A, Ni Y, Saewert M, DeSilva B, Pillutla R.

J Immunol Methods. 2015 Apr;419:18-24. doi: 10.1016/j.jim.2015.02.009. Epub 2015 Feb 27.

PMID:
25728474
11.

Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.

Wacker DA, Wang Y, Broekema M, Rossi K, O'Connor S, Hong Z, Wu G, Malmstrom SE, Hung CP, LaMarre L, Chimalakonda A, Zhang L, Xin L, Cai H, Chu C, Boehm S, Zalaznick J, Ponticiello R, Sereda L, Han SP, Zebo R, Zinker B, Luk CE, Wong R, Everlof G, Li YX, Wu CK, Lee M, Griffen S, Miller KJ, Krupinski J, Robl JA.

J Med Chem. 2014 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v. Epub 2014 Sep 10.

PMID:
25208139
12.

Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.

Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG.

J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12.

PMID:
24521299
13.

Factors influencing magnitude and duration of target inhibition following antibody therapy: implications in drug discovery and development.

Chimalakonda AP, Yadav R, Marathe P.

AAPS J. 2013 Jul;15(3):717-27. doi: 10.1208/s12248-013-9477-3. Epub 2013 Apr 16.

14.

Evaluation of six proton pump inhibitors as inhibitors of various human cytochromes P450: focus on cytochrome P450 2C19.

Zvyaga T, Chang SY, Chen C, Yang Z, Vuppugalla R, Hurley J, Thorndike D, Wagner A, Chimalakonda A, Rodrigues AD.

Drug Metab Dispos. 2012 Sep;40(9):1698-711. doi: 10.1124/dmd.112.045575. Epub 2012 May 30.

PMID:
22648560
15.

Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential.

Kim S, Pray D, Zheng M, Morgan DG, Pizzano JG, Zoeckler ME, Chimalakonda A, Sinz MW.

Drug Metab Lett. 2008 Aug;2(3):169-75.

PMID:
19356089
16.
17.

Attenuation of acute rejection in a rat liver transplantation model by a liver-targeted dextran prodrug of methylprednisolone.

Chimalakonda AP, Montgomery DL, Weidanz JA, Shaik IH, Nguyen JH, Lemasters JJ, Kobayashi E, Mehvar R.

Transplantation. 2006 Mar 15;81(5):678-85.

19.

Hepatic disposition of cyclosporine A in isolated perfused rat livers.

Mehvar R, Chimalakonda AP.

J Pharm Pharm Sci. 2004 Feb 17;7(1):47-54.

22.

Microsomal cytochrome P450 levels and activities of isolated rat livers perfused with albumin.

Vuppugalla R, Shah RB, Chimalakonda AP, Fisher CW, Mehvar R.

Pharm Res. 2003 Jan;20(1):81-8.

PMID:
12608540
23.

High-performance liquid chromatographic analysis of cyclosporin A in rat blood and liver using a commercially available internal standard.

Chimalakonda AP, Shah RB, Mehvar R.

J Chromatogr B Analyt Technol Biomed Life Sci. 2002 May 25;772(1):107-14.

PMID:
12016021

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