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Promiscuous binders

However, these compounds and the fragments are not without their intrinsic problems and should not be used as is. Some examples of potentially problematic compounds include those with chemically reactive groups, dyes, and fluorescent compounds which interfere with assays, frequent hitters/promiscuous binders, and inorganic complexes (55). It is important, then, to a priori filter out such compounds or reagents which are practically useless from a drug discovery point of view. [Pg.159]

Another source of false positive hits is promiscuous binders, which were shown by McGovern et al. [23-26], via dynamic light scattering, to form aggregates above... [Pg.326]

Figure 13.14 Projection of two promiscuous binders, Sertindole (primary target 5-HT2a, left) and Clozapine (primary target D4.2, right), onto the COBRA SOM. The distribution of known serotonin receptor ligands is shown in the left map, the distribution of known dopamine receptor ligands is shown in the right map. The colored areas of the two maps overlap, indicating similar activity of the compounds. Blue few compounds red many compounds crosses indicate unpopulated areas of pharmacophore space. Figure 13.14 Projection of two promiscuous binders, Sertindole (primary target 5-HT2a, left) and Clozapine (primary target D4.2, right), onto the COBRA SOM. The distribution of known serotonin receptor ligands is shown in the left map, the distribution of known dopamine receptor ligands is shown in the right map. The colored areas of the two maps overlap, indicating similar activity of the compounds. Blue few compounds red many compounds crosses indicate unpopulated areas of pharmacophore space.
Mendgen T, Steuer C, Klein CD. Privileged Scaffolds or Promiscuous Binders A Comparative Study on Rhodanines and Related Heterocycles in Medicinal Chemistry. /. Med. Ghent. 2012, 55, 743-753. [Pg.62]


See other pages where Promiscuous binders is mentioned: [Pg.394]    [Pg.20]    [Pg.327]    [Pg.369]    [Pg.371]    [Pg.535]    [Pg.60]    [Pg.124]    [Pg.126]    [Pg.466]    [Pg.20]    [Pg.16]    [Pg.394]    [Pg.20]    [Pg.327]    [Pg.369]    [Pg.371]    [Pg.535]    [Pg.60]    [Pg.124]    [Pg.126]    [Pg.466]    [Pg.20]    [Pg.16]    [Pg.208]    [Pg.163]    [Pg.176]    [Pg.231]    [Pg.270]    [Pg.282]    [Pg.253]    [Pg.541]    [Pg.478]    [Pg.131]   
See also in sourсe #XX -- [ Pg.290 , Pg.394 ]




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