{"id":3835,"date":"2015-04-23T08:23:27","date_gmt":"2015-04-23T08:23:27","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/poster\/ftsa-spr-identifying-small-molecule-ligands-pains\/"},"modified":"2025-12-12T11:34:19","modified_gmt":"2025-12-12T11:34:19","slug":"ftsa-spr-identifying-small-molecule-ligands-pains","status":"publish","type":"poster","link":"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/ftsa-spr-identifying-small-molecule-ligands-pains\/","title":{"rendered":"FTSA and SPR for identifying small molecule ligands and PAINs"},"content":{"rendered":"

Abstract<\/strong><\/p>\n

Biophysical methods are attractive techniques in drug discovery, for both primary screening and orthogonal validation of hits. Here we describe a\u00a0dual method, employing Fluorescent Thermal Shift assay (FTSA<\/a>) and\u00a0surface plasmon resonance (SPR), to interrogate ligands of the kinase p38\u03b1 as well as several known pan-assay interference compounds (PAINs).<\/p>\n

This combinatorial approach allows for independent verification of\u00a0biophysical parameters such as KD, kon, koff, \u0394G, \u0394S, and \u0394H, which may further guide chemical development of a ligand series. Affinity values\u00a0obtained from FTSA curves allow for insight into compound binding.\u00a0Ligand\u2013p38 interaction data were in good agreement with previous\u00a0literature.\u00a0Aggregators and Fluorescence quenchers appeared to reduce Fluorescence signal in the FTSAs, causing artificially high shifts in Tm values,\u00a0whereas redox compounds caused either a depression of FTSA signal or
\nshifts in affinity that did not agree between FTSA and SPR.<\/p>\n","protected":false},"excerpt":{"rendered":"

The power of biophysical methods in drug discovery, utilising FTSA and SPR to validate kinase p38\u03b1 ligands and screen PAINs compounds.<\/p>\n","protected":false},"featured_media":2449,"template":"","category":[1],"class_list":["post-3835","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-uncategorized"],"acf":[],"yoast_head":"\nFTSA & SPR: Identifying Small Molecule Ligands & PAINs<\/title>\n<meta name=\"description\" content=\"Independent KD, kon and koff values from fluorescent thermal shift and surface plasmon resonance, applied to p38\u03b1 ligands and PAINs compounds. 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