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Hit-to-lead

Some types of screens used in hit to lead are controversial and are used in some organizations but not in others. Examples of these are ... [Pg.21]

Virtually every competent drug discovery organization has criteria for the transition between hit to lead and lead optimization. Virtually nobody publishes these criteria because the organizations consider them proprietary. By virtue of very fast note taking and a combined effort, a Pfizer colleague and I were able to capture the hit to lead exit criteria from an oral presentation by a medicinal chemist from the AZ organization. The criteria are as they stood in about year 2000.1 do not know if... [Pg.22]

AstraZeneca (year 2000) Generic lead target profile for progressing HTS hits to leads ... [Pg.23]

Keywords NMR, drug discovery, fragment based drug discovery, SAR by NMR, SAR by ILOEs, hit to lead... [Pg.125]

Gillespie P, Goodnow RA Jr (2004) The hit-to-lead process in drug discovery. In Doherty A (ed) Annual reports in medicinal chemistry. Elsevier, Oxford, p 293... [Pg.171]

As mentioned in Sect. 3, it is important to establish a detailed lead profile at the beginning of a lead identification effort. Criteria vary in different lead identification or hit-to-lead groups, but generally include some or all of the following potency, functional activity, selectivity, MW, clogP, solubility, permeability, microsomal stability and/or hepatocyte clearance, and preliminary PK including oral bioavail-ability. An example of a lead profile for a kinase inhibitor project is illustrated in Table 1 [21],... [Pg.182]

The objective of this volume is to provide an overview of the hit-to-lead process it is not intended to be all inclusive. Furthermore, much of the methodology described here is influenced by the culture of the authors respective institutions. In general, however, lead seeking approaches across industry (and academia) are more similar than they are different and are, for the most part, captured in this volume. [Pg.225]

Overview of Hit to Lead The Medicinal Chemist s Role from HTS Retest to Lead Optimization Hand Off. 1... [Pg.226]

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See also in sourсe #XX -- [ Pg.125 ]



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Affinity-Based Screening Methodologies and Their Application in the Hit-to-Lead Phase

Chemoinformatic Tools for Library Design and the Hit-to-Lead Process A Users Perspective

Early Optimization or Hit-to-Lead Libraries

Filtering hits to leads

Hit to Lead also Known as Closed Loop

Hit to lead program

Hit, hits

Hit-to-lead optimization

Hit-to-lead phase

Hit-to-lead process

Hit-to-lead stage

Hit-to-lead strategies

The Hit-to-lead Process

Visualization of Library Designs during Hit-to-lead Efforts

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