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Synergy and antagonism of promiscuous inhibition in multiple-compound mixtures.


ABSTRACT: Screening in mixtures is a common approach for increasing the efficiency of high-throughput screening. Here we investigate how the "compound load" of mixtures influences promiscuous aggregate-based inhibition. We screened 764 molecules individually and in mixtures of 10 at 5 miccroM each, comparing the observed inhibition of the mixtures to that predicted from single-compound results. Synergistic effects on aggregation predominated, although antagonism was also observed. These results suggest that screening mixtures can increase aggregation-based inhibition in a nonadditive manner.

SUBMITTER: Feng BY 

PROVIDER: S-EPMC1540993 | biostudies-literature | 2006 Apr

REPOSITORIES: biostudies-literature

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Synergy and antagonism of promiscuous inhibition in multiple-compound mixtures.

Feng Brian Y BY   Shoichet Brian K BK  

Journal of medicinal chemistry 20060401 7


Screening in mixtures is a common approach for increasing the efficiency of high-throughput screening. Here we investigate how the "compound load" of mixtures influences promiscuous aggregate-based inhibition. We screened 764 molecules individually and in mixtures of 10 at 5 miccroM each, comparing the observed inhibition of the mixtures to that predicted from single-compound results. Synergistic effects on aggregation predominated, although antagonism was also observed. These results suggest th  ...[more]

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