Abstract
The fast pace of drug discovery programs, aided by high-throughput screening campaigns, often relies on the generation of combinatorial libraries to identify new chemical entities. The Ugi 4- and 3-component reactions in particular [1], have proven to be robust in producing both tool compounds and drugs [2,3]. Here we report a high-throughput entry into the imidazopyridine scaffold, using a microfluidic-assisted synthesis setup, coupled to a target prediction tool to de-orphan a focused compound library with high success rate, and identify an innovative GPCR-inhibiting chemotype. Combinatorial compounds were correctly identified as ligand-efficient adenosine A1/2B, and adrenergic α1A/B inhibitors with Ki values in the low micromolar range.
Highlights
The fast pace of drug discovery programs, aided by highthroughput screening campaigns, often relies on the generation of combinatorial libraries to identify new chemical entities
We report a high-throughput entry into the imidazopyridine scaffold, using a microfluidic-assisted synthesis setup, coupled to a target prediction tool to de-orphan a focused compound library with high success rate, and identify an innovative GPCR-inhibiting chemotype
Combinatorial compounds were correctly identified as ligand-efficient adenosine A1/2B, and adrenergic a1A/B inhibitors with Ki values in the low micromolar range
Summary
The fast pace of drug discovery programs, aided by highthroughput screening campaigns, often relies on the generation of combinatorial libraries to identify new chemical entities.
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