Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.

Autor: Brough PA; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Baker L; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Bedford S; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Brown K; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Chavda S; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Chell V; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., D'Alessandro J; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Davies NG; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Davis B; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Le Strat L; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Macias AT; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Maddox D; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Mahon PC; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Massey AJ; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Matassova N; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., McKenna S; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Meissner JW; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Moore JD; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Murray JB; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Northfield CJ; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Parry C; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Parsons R; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Roughley SD; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Shaw T; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Simmonite H; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Stokes S; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Surgenor A; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Stefaniak E; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Robertson A; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Wang Y; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Webb P; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Whitehead N; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K., Wood M; Vernalis (R&D) Ltd. , Granta Park, Great Abington, Cambridge CB21 6GB, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Mar 23; Vol. 60 (6), pp. 2271-2286. Date of Electronic Publication: 2017 Feb 15.

Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.

Autor: Watson RJ; UCB Inflammation Discovery, Granta Park, Great Abington, Cambridge CB21 6GS, United Kingdom. bob.watson@ucb-group.com, Allen DR, Birch HL, Chapman GA, Galvin FC, Jopling LA, Knight RL, Meier D, Oliver K, Meissner JW, Owen DA, Thomas EJ, Tremayne N, Williams SC

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 01; Vol. 18 (1), pp. 147-51. Date of Electronic Publication: 2007 Nov 04.

Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Autor: Alam M; UCB, Granta Park, Great Abington, Cambridge CB21 6GS, UK., Beevers RE, Ceska T, Davenport RJ, Dickson KM, Fortunato M, Gowers L, Haughan AF, James LA, Jones MW, Kinsella N, Lowe C, Meissner JW, Nicolas AL, Perry BG, Phillips DJ, Pitt WR, Platt A, Ratcliffe AJ, Sharpe A, Tait LJ

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jun 15; Vol. 17 (12), pp. 3463-7. Date of Electronic Publication: 2007 Mar 30.

Synthesis and structure-activity relationships of guanine analogues as phosphodiesterase 7 (PDE7) inhibitors.

Autor: Barnes MJ; Celltech R & D, Granta Park, Great Abington, Cambridge, UK., Cooper N, Davenport RJ, Dyke HJ, Galleway FP, Galvin FC, Gowers L, Haughan AF, Lowe C, Meissner JW, Montana JG, Morgan T, Picken CL, Watson RJ

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Apr 23; Vol. 11 (8), pp. 1081-3.

Use of Quantitative Structure--Activity Relationship (QSAR) and ADMET prediction studies as screening methods for design of benzyl urea derivatives for anti-cancer activity.

Autor: Lokwani, Deepak¹ (AUTHOR), Bhandari, Shashikant¹ (AUTHOR) drugdesign1@gmail.com, Pujari, Radha² (AUTHOR), Shastri, Padma² (AUTHOR), shelke, Ganesh² (AUTHOR), Pawar, Vidya¹ (AUTHOR)

Publikováno v: Journal of Enzyme Inhibition & Medicinal Chemistry. Jun2011, Vol. 26 Issue 3, p319-331. 13p.