Tackling MedChem Bias One Functional Group at a Time
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In this Flash Talk, Yoshihiro Ishihara discussed the beneficial effects of chloro and methoxy substituents on intermolecular interactions, as well as the unique advantages and disadvantages of employing these substituents in drug discovery.
As part of our Flash Talk webinar series, we present a PDF of Yoshihiro Ishihara's slide deck and full text questions and answers from his talk, entitled "Roles of the Chloro and Methoxy Groups in Drug Discovery." Check out the recording of the talk on our Drug Hunter YouTube channel.
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Olutasidenib: Potentially Longer Complete Remissions in AML with a Second-Generation IDH1 Inhibitor
Olutasidenib, discovered by Forma Therapeutics and marketed by Rigel, is an oral, brain-penetrant, selective mIDH1 inhibitor. It was granted Orphan Drug Designation and approved in December 2022 by the FDA for adults with relapsed/refractory acute myeloid leukemia. Approval was granted based on a Ph. I/II trial showing a 35% CR+CRh rate and a favorable 25.9-month median duration. This article describes the discovery and development of olutasidenib, how it is distinct from other mIDH inhibitors, and its potential in treating gliomas.
Computational Partnership in Small Molecule Drug Discovery
The real magic happens when chemists can integrate computational models into their assay cascades, thanks to trust in their predictions. To get there, grounding computational predictions in physics and experimental reality makes all the difference. In this article, Abba E. Leffler, Ph.D. from Schrödinger tells us about: How to make [...]
