The reemergence of covalent compounds: Domainex’s approach to covalent fragment screening

In the fourth of our Drug Discovery webinar series, we discussed covalent fragment screening and its reemerging promise in drug discovery. The series was hosted by One Nucleus.

Covalent inhibitors have reemerged as a hot topic in drug discovery research. During this webinar, we discussed our approach to identifying high quality covalent fragment hits. This included curation of our diverse covalent fragment library, covalent fragment screening by intact mass spectrometry, assessment of warhead reactivity with glutathione (GSH), confirmation of the fragment binding site by peptide mapping and generation of Ki/kinact values by LC-MS.

Agenda:

• Introduction from One Nucleus and Domainex
• Presentation from Andrew Ratcliffe, Head of Chemistry and Scott Martin, Head of the Bioanalytical Sciences Department, Domainex
• Q&A and Close