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Improving the hit-to-lead process: data-driven assessment of drug-like and lead-like screening hits
Wunberg T, Hendrix M, Hillisch A, Lobell M, Meier H, Schmeck C, Wild H and Hinzen B
Drug Discovery Today
Drug-like and lead-like hits derived from HTS campaigns provide good starting points for lead
optimization. However, too strong emphasis on potency as hit-selection parameter might hamper the
success of such projects. A detailed absorption, distribution, metabolism, excretion and toxicology
(ADME–Tox) profiling is needed...
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Abstracts
of Key Research Articles
Components of successful lead generation
Davis AM, Keeling DJ, Steele J, Tomkinson NP and Tinker AC
Curr. Top. Med. Chem. 2005; 5; 421–439
High-throughput screening-driven lead discovery: meeting the challenges of finding new therapeutics
Posner BA
Curr. Opin. Drug Discov. Devel. 2005; 8; 487-494
The influence of drug-like concepts on decision making in medicinal chemistry
Leeson PD and Springthorpe B
Nat. Rev. Drug Discov. 2007; 6; 881–890
Fragment-based drug design: combining philosophy with technology
Bartoli S, Fincham CI and Fattori D
Curr. Opin. Drug Discov. Devel. 2007; 10; 422–429
Synthetic library design
Huwe CM
Drug Discov. Today 2006; 11; 763–767
Tools for efficient high-throughput synthesis
Chighine A, Sechi G and Bradley M
Drug Discov. Today 2007; 12; 459–464
Scaffold selection and scaffold hopping in lead generation: a medicinal chemistry perspective
Zhao H
Drug Discov. Today 2007; 12 149–155
The discovery of CCR5 receptor antagonists for the treatment of HIV infection: hit-to-lead studies
Armour D, de Groot MJ, Edwards M, Perros M, Price DA, Stammen BL and Wood A
ChemMedChem 2006; 1; 706–709
Rapid hit to lead evaluation of pyrazolo[3,4-d-pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists
Wang X, Kolasa T, El Kouhen OF, Chovan LE, Black-Shaefer CL, Wagenaar FL, Garton JA, Moreland RB, Honore P, Lau YY, Dandliker PJ, Brioni JD and Stewart AO
Bioorg. Med. Chem. Lett. 2007; 17; 4303–4307
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies
Morwick T, Berry A, Brickwood J, Cardozo M, Catron K, DeTuri M, Emeigh J, Homon C, Hrapchak M, Jacober S, Jakes S, Kaplita P, Kelly TA, Ksiazek J, Liuzzi M, Magolda R, Mao C, Marshall D, McNeil D, Prokopowicz A 3rd, Sarko C, Scouten E, Sledziona C, Sun S, Watrous J, Wu JP and Cywin CL
J. Med. Chem. 2006; 49; 2898–2908 |
