{"entity": "researcher", "timestamp": "2026-09-08T10:39:46.824Z", "family": "Vallin", "given": "Michaela", "initials": "M", "orcid": "0000-0001-5103-492X", "affiliations": ["Chemical Biology Consortium Sweden, Science for Life Laboratory , Karolinska Institutet , SE-171 65 Solna , Sweden.", "Department of Medical Biochemistry and Biophysics , Karolinska Institutet , SE-171 65 Solna , Sweden."], "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/researcher/e914ecc1df1a4266988a72890de65cb5.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/researcher/e914ecc1df1a4266988a72890de65cb5"}}, "publications": [{"entity": "publication", "iuid": "18a363c725db436884d8763754177aa2", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/18a363c725db436884d8763754177aa2.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/18a363c725db436884d8763754177aa2"}}, "title": "In Situ Target Engagement Studies in Adherent Cells.", "authors": [{"family": "Axelsson", "given": "Hanna", "initials": "H", "orcid": "0000-0003-2365-1749", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/affc5ee12a2d47b6a7f9ab3df049991e.json"}}, {"family": "Almqvist", "given": "Helena", "initials": "H"}, {"family": "Otrocka", "given": "Magdalena", "initials": "M"}, {"family": "Vallin", "given": "Michaela", "initials": "M", "orcid": "0000-0001-5103-492X", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/e914ecc1df1a4266988a72890de65cb5.json"}}, {"family": "Lundqvist", "given": "Sara", "initials": "S"}, {"family": "Hansson", "given": "Pia", "initials": "P"}, {"family": "Karlsson", "given": "Ulla", "initials": "U"}, {"family": "Lundb\u00e4ck", "given": "Thomas", "initials": "T"}, {"family": "Seashore-Ludlow", "given": "Brinton", "initials": "B", "orcid": "0000-0001-8658-5967", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/8a8ea4c3fdb14de1b651d0367b0a70a4.json"}}], "type": "journal article", "published": "2018-04-20", "journal": {"title": "ACS chemical biology", "issn": "1554-8937", "volume": "13", "issue": "4", "pages": "942-950", "issn-l": "1554-8929"}, "abstract": "A prerequisite for successful drugs is effective binding of the desired target protein in the complex environment of a living system. Drug-target engagement has typically been difficult to monitor in physiologically relevant models, and with current methods, especially, while maintaining spatial information. One recent technique for quantifying drug-target engagement is the cellular thermal shift assay (CETSA), in which ligand-induced protein stabilization is measured after a heat challenge. Here, we describe a CETSA protocol in live A431 cells for p38\u03b1 (MAPK14), where remaining soluble protein is detected in situ, using high-content imaging in 384-well, microtiter plates. We validate this assay concept using a number of known p38\u03b1 inhibitors and further demonstrate the potential of this technology for chemical probe and drug discovery purposes by performing a small pilot screen for novel p38\u03b1 binders. Importantly, this protocol creates a workflow that is amenable to adherent cells in their native state and yields spatially resolved target engagement information measurable at the single-cell level.", "doi": "10.1021/acschembio.7b01079", "pmid": "29433316", "labels": [], "xrefs": [], "notes": [], "created": "2018-12-05T12:41:55.229Z", "modified": "2026-08-21T11:35:40.142Z"}]}