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Jayvardhan Pandit

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Mark S Plummer; Howard Roark; Nalini Sadagopan; Brian Sanchez; Ron Sarver; Aurash B Shahripour; Xi Qiang Shen; Donald J Skalitzky; Cindy Spessard; Charles J Stankovic; Katherine Welch; Christopher Whitehead; Craig Banotai; Heidi Baum; David Beidler; Susan E Bove; Timothy Braden; Joseph Cornicelli; Annise Goodman; Richard C Gowan; James Hicks; Xiao Kang Lu; Howard Miller; Adam Ogden; Jayvardhan Pandit; Sandra Lightle
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: Optimization studies and demonstration of in vivo efficacy.
Mark S Plummer; Howard Roark; Nalini Sadagopan; Brian Sanchez; Ron Sarver; Aurash B Shahripour; Xi Qiang Shen; Donald J Skalitzky; Cindy Spessard; Charles J Stankovic; Katherine Welch; Christopher Whitehead; Craig Banotai; Heidi Baum; David Beidler; Susan E Bove; Timothy Braden; Joseph Cornicelli; Annise Goodman; Richard C Gowan; James Hicks; Xiao Kang Lu; Howard Miller; Adam Ogden; Jayvardhan Pandit; Sandra Lightle
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, Part I: Transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
Amy B Dounay; Edelweiss Evrard; Xinmin Gan; Ji-Young Kim; Laura A McAllister; Jayvardhan Pandit; Suobao Rong; Michelle A Salafia; Jamison B Tuttle; Marie Anderson; Bruce M Bechle; Laura E Zawadzke; Patrick R Verhoest
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.

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All Publications

2013: Mark S Plummer; Howard Roark; Nalini Sadagopan; Brian Sanchez; Ron Sarver; Aurash B Shahripour; Xi Qiang Shen; Donald J Skalitzky; Cindy Spessard; Charles J Stankovic; Katherine Welch; Christopher Whitehead; Craig Banotai; Heidi Baum; David Beidler; Susan E Bove; Timothy Braden; Joseph Cornicelli; Annise Goodman; Richard C Gowan; James Hicks; Xiao Kang Lu; Howard Miller; Adam Ogden; Jayvardhan Pandit; Sandra Lightle
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: Optimization studies and demonstration of in vivo efficacy.
Bioorganic & medicinal chemistry letters 2013;23(11):3443-7.
2013: Mark S Plummer; Howard Roark; Nalini Sadagopan; Brian Sanchez; Ron Sarver; Aurash B Shahripour; Xi Qiang Shen; Donald J Skalitzky; Cindy Spessard; Charles J Stankovic; Katherine Welch; Christopher Whitehead; Craig Banotai; Heidi Baum; David Beidler; Susan E Bove; Timothy Braden; Joseph Cornicelli; Annise Goodman; Richard C Gowan; James Hicks; Xiao Kang Lu; Howard Miller; Adam Ogden; Jayvardhan Pandit; Sandra Lightle
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, Part I: Transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
Bioorganic & medicinal chemistry letters 2013;23(11):3438-42.
2013: Amy B Dounay; Edelweiss Evrard; Xinmin Gan; Ji-Young Kim; Laura A McAllister; Jayvardhan Pandit; Suobao Rong; Michelle A Salafia; Jamison B Tuttle; Marie Anderson; Bruce M Bechle; Laura E Zawadzke; Patrick R Verhoest
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.
Bioorganic & medicinal chemistry letters 2013;23(7):1961-6.
2013: Frank S Menniti; Jayvardhan Pandit; P Jeffrey Conn; Craig W Lindsley; Panayiotis Zagouras; Robert A Volkmann
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks.
Current topics in medicinal chemistry 2013;13(1):26-54.
2012: Ivan V Efremov; Steven W Goldstein; Mahmoud Mansour; Alexander McColl; Stephen Noell; Christine E Oborski; Thomas N O'Connell; Theresa J O'Sullivan; Jayvardhan Pandit; Felix F Vajdos; Hong Wang; Binqing Wei; Kris A Borzilleri; Steven Capetta; Hou Chen; Peter H Dorff; Jason K Dutra; Jane M Withka
Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design.
Journal of medicinal chemistry 2012;55(21):9069-88.
2011: Christopher J Helal; Xinjun Hou; John M Humphrey; Zhijun Kang; Lorraine A Lebel; Douglas S Chapin; Thomas A Chappie; Lois K Chenard; Julie Cianfrogna; Kimberly F Fennell; Kari R Fonseca; Carol Fox; Mary MacDougall; Eric S Marr; Laura McDowell; Frank Menniti; Frederick R Nelson; Rebecca O'Connor; Jayvardhan Pandit; Christopher J Schmidt; Judith Siuciak; Robert D Williams; Spiros Liras
Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.
Journal of medicinal chemistry 2011;54(13):4536-47.
2011: Karen Coffman; Michael Brodney; James Cook; Lorraine Lanyon; Jayvardhan Pandit; Subas M Sakya; Joel Schachter; Elaine Tseng-Lovering; Matthew Wessel
6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(5):1429-33.
2010: Kevin D Freeman-Cook; Christopher Autry; Gary Borzillo; Deborah Gordon; Elsa Barbacci-Tobin; Vincent Bernardo; David Briere; Tracey Clark; Matthew Corbett; John Jakubczak; Shefali Kakar; Elizabeth Knauth; Blaise Lippa; Michael J Luzzio; Mahmoud Mansour; Gary Martinelli; Matthew Marx; Kendra Nelson; Jayvardhan Pandit; Francis Rajamohan; Shaughnessy Robinson; Chakrapani Subramanyam; Liuqing Wei; Martin Wythes; Joel Morris
Design of selective, ATP-competitive inhibitors of Akt.
Journal of medicinal chemistry 2010;53(12):4615-22.
2009: Clemens C Heikaus; Jayvardhan Pandit; Rachel E Klevit
Cyclic nucleotide binding GAF domains from phosphodiesterases: structural and mechanistic insights.
Structure (London, England : 1993) 2009;17(12):1551-7.
2009: Jayvardhan Pandit; Michael D Forman; Kimberly F Fennell; Keith S Dillman; Frank S Menniti
Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(43):18225-30.
2009: Patrick R Verhoest; Douglas S Chapin; Michael Corman; Kari Fonseca; John F Harms; Xinjun Hou; Eric S Marr; Frank Menniti; Frederick Nelson; Rebecca O'Connor; Jayvardhan Pandit; Caroline Proulx-Lafrance; Anne W Schmidt; Christopher J Schmidt; Judith A Suiciak; Spiros Liras
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.
Journal of medicinal chemistry 2009;52(16):5188-96.
2008: Blaise Lippa; Gonghua Pan; Matthew Corbett; Chao Li; Goss S Kauffman; Jayvardhan Pandit; Shaughnessy Robinson; Liuqing Wei; Ekaterina Kozina; Eric S Marr; Gary Borzillo; Elisabeth Knauth; Elsa G Barbacci-Tobin; Patrick Vincent; Merin Troutman; Deborah Baker; Francis Rajamohan; Shefali Kakar; Tracey Clark; Joel Morris
Synthesis and structure based optimization of novel Akt inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(11):3359-63.
2007: Kevin D Freeman-Cook; Lawrence A Reiter; Mark C Noe; Amy S Antipas; dennis danley; Kaushik Datta; James T Downs; Shane Eisenbeis; James D Eskra; David J Garmene; Elaine M Greer; Richard J Griffiths; Roberto Guzman; Joel R Hardink; Fouad Janat; Christopher S Jones; Gary J Martinelli; Peter G Mitchell; Ellen R Laird; Jennifer L Liras; Lori L Lopresti-Morrow; Jayvardhan Pandit; Usa D Reilly; Donald Robertson; Marcie L Vaughn-Bowser; Lilli A Wolf-Gouviea; Sue A Yocum
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.
Bioorganic & medicinal chemistry letters 2007;17(23):6529-34.
2007: Felix F Vajdos; Lise R Hoth; Kieran F Geoghegan; Samuel P Simons; Peter K LeMotte; dennis danley; Mark J Ammirati; Jayvardhan Pandit
The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene.
Protein science : a publication of the Protein Society 2007;16(5):897-905.
2007: Thomas A Chappie; John M Humphrey; Martin P Allen; Kimberly G Estep; Carol B Fox; Lorraine A Lebel; Spiros Liras; Eric S Marr; Frank S Menniti; Jayvardhan Pandit; Christopher J Schmidt; Meihua Tu; Robert D Williams; Feng V Yang
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
Journal of medicinal chemistry 2007;50(2):182-5.
2006: Lawrence A Reiter; Kevin D Freeman-Cook; Christopher S Jones; Gary J Martinelli; Amy S Antipas; Martin A Berliner; Kaushik Datta; James T Downs; James D Eskra; Michael D Forman; Elaine M Greer; Roberto Guzman; Joel R Hardink; Fouad Janat; Nandell F Keene; Ellen R Laird; Jennifer L Liras; Lori L Lopresti-Morrow; Peter G Mitchell; Jayvardhan Pandit; Donald Robertson; Diana Sperger; Marcie L Vaughn-Bowser; Darra M Waller; Sue A Yocum
Potent, selective pyrimidinetrione-based inhibitors of MMP-13.
Bioorganic & medicinal chemistry letters 2006;16(22):5822-6.
2005: Kim F McClure; Yuriy A Abramov; Ellen R Laird; John T Barberia; Weiling Cai; Thomas J Carty; Santo R Cortina; dennis danley; Alan J Dipesa; Kathleen M Donahue; Mark A Dombroski; Nancy C Elliott; Christopher A Gabel; Seungil Han; THOMAS HYNES; Peter K LeMotte; Mahmoud N Mansour; Eric S Marr; Michael A Letavic; Jayvardhan Pandit; David B Ripin; Francis J Sweeney; Douglas Tan; Yong Tao
Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.
Journal of medicinal chemistry 2005;48(18):5728-37.
2005: Julian A Blagg; Mark C Noe; Lilli A Wolf-Gouveia; Lawrence A Reiter; Ellen R Laird; Shang-Poa P Chang; dennis danley; James T Downs; Nancy C Elliott; James D Eskra; Richard J Griffiths; Joel R Hardink; Amber I Haugeto; Christopher S Jones; Jennifer L Liras; Lori L Lopresti-Morrow; Peter G Mitchell; Jayvardhan Pandit; Ralph P Robinson; Chakrapani Subramanyam; Marcie L Vaughn-Bowser; Sue A Yocum
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Bioorganic & medicinal chemistry letters 2005;15(7):1807-10.
2003: Stephen W Wright; Anthony A Carlo; dennis danley; David L Hageman; George A Karam; Mahmoud N Mansour; Lester D McClure; Jayvardhan Pandit; Gayle K Schulte; Judith L Treadway; Ing-Kae Wang; Paul H Bauer
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site.
Bioorganic & medicinal chemistry letters 2003;13(12):2055-8.
2003: Robert L Dow; Steven R Schneider; Ernest S Paight; Richard F Hank; Phoebe Chiang; Peter Cornelius; Eunsun Lee; William P Newsome; Andrew G Swick; Josephine Spitzer; Diane M Hargrove; Terrell A Patterson; Jayvardhan Pandit; Boris A Chrunyk; Peter K LeMotte; dennis danley; Michele H Rosner; Mark J Ammirati; Samuel P Simons; Gayle K Schulte; Barbara Tate; Paul DaSilva-Jardine
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.
Bioorganic & medicinal chemistry letters 2003;13(3):379-82.
2002: Stephen W Wright; Anthony A Carlo; Maynard D Carty; dennis danley; David L Hageman; George A Karam; Carolyn B Levy; Mahmoud N Mansour; Alan M Mathiowetz; Lester D McClure; Nestor B Nestor; R Kirk McPherson; Jayvardhan Pandit; Leslie R Pustilnik; Gayle K Schulte; Walter Soeller; Judith L Treadway; Ing-Kae Wang; Paul H Bauer
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography.
Journal of medicinal chemistry 2002;45(18):3865-77.
2002: Michael A Letavic; Matt Z Axt; John T Barberia; Thomas J Carty; dennis danley; Kieran F Geoghegan; Nadia S Halim; Lise R Hoth; Ajith V Kamath; Ellen R Laird; Lori L Lopresti-Morrow; Kim F McClure; Peter G Mitchell; Vijayalakshmi Natarajan; Mark C Noe; Jayvardhan Pandit; Lisa M Reeves; Gayle K Schulte; Sheri L Snow; Francis J Sweeney; Douglas H Tan; Chul H Yu
Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.
Bioorganic & medicinal chemistry letters 2002;12(10):1387-90.
2000: Jayvardhan Pandit; dennis danley; Gayle K Schulte; S Mazzalupo; Thomas A Pauly; C M Hayward; E S Hamanaka; J F Thompson; H J Harwood
Crystal structure of human squalene synthase. A key enzyme in cholesterol biosynthesis.
The Journal of biological chemistry 2000;275(39):30610-7.
2000: Philip G Board; Marjorie Coggan; G Chelvanayagam; Simon Easteal; Lars S Jermiin; Gayle K Schulte; dennis danley; Lise R Hoth; Matthew C Griffor; A V Kamath; Michele H Rosner; Boris A Chrunyk; D E Perregaux; Christopher A Gabel; Kieran F Geoghegan; Jayvardhan Pandit
Identification, characterization, and crystal structure of the Omega class glutathione transferases.
The Journal of biological chemistry 2000;275(32):24798-806.
2000: Virginia L Rath; Mark J Ammirati; Peter K LeMotte; K F Fennell; Mahmoud N Mansour; dennis danley; THOMAS HYNES; Gayle K Schulte; D J Wasilko; Jayvardhan Pandit
Activation of human liver glycogen phosphorylase by alteration of the secondary structure and packing of the catalytic core.
Molecular cell 2000;6(1):139-48.
1999: Lawrence A Reiter; J P Rizzi; Jayvardhan Pandit; M J Lasut; S M McGahee; V D Parikh; James F Blake; dennis danley; Ellen R Laird; Arturo Lopez-Anaya; Lori L Lopresti-Morrow; Mahmoud N Mansour; Gary J Martinelli; Peter G Mitchell; B S Owens; Thomas A Pauly; Lisa M Reeves; Gayle K Schulte; Sue A Yocum
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.
Bioorganic & medicinal chemistry letters 1999;9(2):127-32.