Chemical Biology

Highthroughput Binder Confirmation (HTBC): A new non-combinatorial synthesis platform created to enhance and accelerate hit ID.

Tuesday, February 6
3:00 PM - 3:30 PM
Location: 8

Sponsored By 

Highthroughput Binder Confirmation (HTBC): A new non-combinatorial synthesis platform created to enhance and accelerate hit ID.
Joseph Franklin, Xiaopeng Bai, Lijun Fan, Kenneth Lind, Heather O’Keefe, Eric Shi, Jennifer Summerfield, Jerry Yap & Jeffrey Messer
NCE Molecular Discovery - GSK

Encoded Library Technology (ELT) is a hit identification platform that uses ultra-large collections of chemically diverse DNA-encoded small molecule libraries selected for affinity against a therapeutically relevant target. Recent advances in ELT libraries, library pooling strategies, selections and DNA sequencing have vastly increased the number of actionable chemotypes produced for a given selection campaign. In practice, only a small fraction of these chemotypes are synthesized as discrete molecules without the encoding DNA using traditional organic synthesis. To address this bottleneck we developed an automated microscale parallel synthesis platform that uses double stranded DNA with a cleavable linker as a chemical handle. This High Throughput Binder Confirmation (HTBC) platform uses the original DNA-Encoded Library (DEL) chemistry and will recapitulate the products, side-products and intermediates produced in the original library synthesis. The resulting compounds are cleaved from the DNA support and are screened as small molecule mixtures by Affinity Selection Mass Spectrometry. The platform is capable of assessing target engagement for hundreds of compounds per month and is used at GSK to prioritize synthesis decisions for more traditional scale organic synthesis.

Joe Franklin

Manager
GlaxoSmithKline

DNA Encoded Library on-DNA chemistry

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Highthroughput Binder Confirmation (HTBC): A new non-combinatorial synthesis platform created to enhance and accelerate hit ID.



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