Lead generation

Aventis Pharma Deutschland GmbH DI A Lead Generation Chemoinfonmatics Industriepark Hoechst, G879 65926 Frankfurt / Main Jaroslaw.Tomczak aventis.com... 

Lead generation natural ligand sereening literature leads... 

DP Mamott, IG Dougall, P Meghani, Y-J Liu, DR Flower. Lead generation using pharmacophore mapping and three-dimensional database searching Application to muscarinic M3 receptor antagonists. J Med Chem 42 3210-3216, 1999. 

The Office of Oceanic and Atmospheric Research (OAR) is the division of NOAA that conducts and directs oceanic and atmospheric research. Since carbon dioxide is a greenhouse gas and fossil fuels are the leading generator of carbon dioxide, the work of the twelve Environmental Research Laboratories and eleven Joint Institutes of OAR to describe, monitor, and assess climate trends are of great interest to all parties interested in the affect of energy use on climate change. 

Fejzo J, Lepre CA, Peng JW et al (1999) The SHAPES strategy an NMR-based approach for lead generation in drag discovery. Chem Biol 6(10) 755-769... 

Davis AM, Keeling DJ, Steele J, Tomkinson NP, Tinker AC. Components of successful lead generation. Curr Top Med Chem 2005 5 421-39. 

One early step in the workflow of the medicinal chemist is to computationally search for similar compounds to known actives that are either available in internal inventory or commercially available somewhere in the world, that is, to perform similarity and substructure searches on the worldwide databases of available compounds. It is in the interest of all drug discovery programs to develop a formal process to search for such compounds and place them into the bioassays for both lead generation and analog-based lead optimization. To this end, various similarity search algorithms (both 2D and 3D) should be implemented and delivered directly to the medicinal chemist. These algorithms often prove complementary to each other in terms of the chemical diversity of the resulted compounds [8]. 

Bleicher KH, Bohm HJ, Muller K, Alanine AI. Hit and lead generation beyond high-throughput screening. Nat Rev Drug Discov 2003 2 369-78. 

Abagyan R. Totrov M. High-throughpnt docking for lead generation. Curr Opin Chem Biol 2001 5 375-82. 

N. NMR experiments for lead generation in drug discovery. Prog. 

Burrows, J. Lead generation by fragment screening. Presented at SCIpharm 2006 International Pharmaceutical Industry Conference, Edinburgh, 2006. 

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Structure-based lead generation, 44 (2006) 1 Synthesis of enantiomers of drugs, 34 (1997) 203... 

A detailed screening pathway starting with a screen to generate hits and culminating in leads is also important for guiding lead generation efforts. An example is illustrated in Fig. 1. 

The following examples taken from the literature since 2001 are intended to illustrate the parallel optimization of some or all of the parameters discussed above, and to illustrate how some of the tools described above can aid in lead generation. It is not meant to be an exhaustive survey of the literature. The specific criteria used to define a successful lead identification campaign vary by group, as do the processes used to reach the lead stage. However, there are also many themes that are common to many of the examples below. A summary of the examples described below is contained in Table 2. 

This kind of shift mapping has been used extensively in NMR studies of protein-ligand interactions. Shuker et al.1/2 used this method to advantage in a lead generation approach that effectively covalently links two... 

Micro-Scaled Lead Generation and Optimisation Systems... 

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