WebNov 19, 2024 · Covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) are described and studies towards a strategy for photocapture of PHD2 substrates are studied. We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of … WebPhotoAffinity. Bits (PhABits) to study protein-ligand. binding. Ross Thomas, University of Strathclyde / GlaxoSmithKline, UK. P26. C–H . functionalisation. tolerant to polar groups could transform FBDD. Chloe . Townley
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WebNov 16, 2024 · Fragment screening offers an efficient approach to explore chemical space. Presented here is a fragment-screening platform, termed PhABits (PhotoAffinity Bits), … WebThe platform enabled the rapid synthesis of >1000 PhotoAffinity Bits (HTC-PhABits) in 384-well plates in 24 h and their subsequent screening as crude reaction products with a protein target without purification. Screening ... a limitation of analysing negative hits from photoaffinity labelling experiments is the potential for false negatives ... on the menu brand
PhotoAffinity Bits: A photoaffinity‐based fragment screening …
WebWe present a fragment screening platform, termed PhABits (PhotoAffinity Bits), which utilises a library of photoreactive fragments to covalently capture fragment-protein interactions. Hits can be profiled to determine potency and site of crosslinking, and subsequently developed as reporters in a competitive displacement assay to identify … WebSep 2, 2024 · Presented here is a fragment-screening platform, termed PhABits (PhotoAffinity Bits), which utilizes a library of photoreactive fragments to covalently capture fragment-protein interactions. Hits can be profiled to determine potency and the site of crosslinking, and subsequently developed as reporters in a competitive displacement … WebPhotoAffinity Bits: A Photoaffinity-Based Fragment Screening Platform for Efficient Identification of Protein Ligands emma grant, david fallon, michael hann, ken fantom, chad quinn, Francesca Zappacosta, Roland S. Annan, Chun-wa Chung, Paul Bamborough, david dixon, peter stacey, David House, Vipulkumar patel, Nicholas C. O. on the mend the broken view