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32-agonists, screening

For the primary screen data, we retain from aU the retrieved percent-of-control values from the database, the minimum values for antagonistic screens and the maximum ones for agonistic screens if multiple measurements per compound and method exist. In this way, we generated up to now approximately 20 million agonist and 150 million antagonist data points. [Pg.303]

GPR81 Human CHO Time Resolved Fluorescence Agonist screen 10 (iM compound concentration... [Pg.600]

Human CHO Second Messenger Time Resolved Fluorescence agonist screen 10 pM compound concentration using same cellular background as primary screen without overexpressing GPR81... [Pg.600]

GPR81 Human CHO agonist screen 7 point concentration response... [Pg.600]

GPR81 Human Membrane lactate Second Messenger Radiometric - Filtration Agonist screen 10 pM compound concentration GTPyS binding assay... [Pg.600]

GPR81 Rat CHO agonist screen 10 point, ensures activity in relevant in vivo species... [Pg.600]

In the GPR81 human CHO lactate second messenger TRF agonist screen, 941439 compounds were tested. The cutoff criterion for an active hit was set to 15%. Corresponding to a hit rate of 0.57%, 5345 primary actives were identified. All actives were retested at 10 pM single concentration in triplicates. In this... [Pg.606]

Fiirst, P., and Bernsmann, T. (2010) High resolution LC-MS beta-agonist screening using turboflow/exactive. Presentation at the 5th Thermo Scientific High Resolution GC-MS Meeting on POPs, Barcelona,... [Pg.351]

Previously, pharmacologists were constrained to the prewired sensitivity of isolated tissues for agonist study. As discussed in Chapter 2, different tissues possess different densities of receptor, different receptor co-proteins in the membranes, and different efficiencies of stimulus-response mechanisms. Judicious choice of tissue type could yield uniquely useful pharmacologic systems (i.e., sensitive screening tissues). However, before the availability of recombinant systems these choices were limited. With the ability to express different densities of human target proteins such as receptors has come a transformation in drug discovery. Recombinant cellular systems can now... [Pg.85]

Heterodimeric receptors, 182t Hetero dimerization, 181 Heterologous desensitization, 34 High-throughput screening agonists, 156 antagonists, 156... [Pg.296]

See other pages where 32-agonists, screening is mentioned: [Pg.156]    [Pg.69]    [Pg.3122]    [Pg.223]    [Pg.223]    [Pg.159]    [Pg.600]    [Pg.635]    [Pg.639]    [Pg.644]    [Pg.129]    [Pg.19]    [Pg.81]    [Pg.133]    [Pg.153]    [Pg.154]    [Pg.155]    [Pg.160]    [Pg.160]    [Pg.183]    [Pg.190]    [Pg.200]    [Pg.238]    [Pg.251]    [Pg.296]    [Pg.299]    [Pg.20]    [Pg.715]    [Pg.715]    [Pg.761]    [Pg.917]    [Pg.1115]    [Pg.1117]    [Pg.198]    [Pg.389]    [Pg.281]    [Pg.118]   
See also in sourсe #XX -- [ Pg.116 , Pg.116 ]



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