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On quality criteria for covalent and degrader probes

Molecular Design

I’ll be taking a look at H2023 (Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes) in this post and this article has also been discussed In The Pipeline. Carefully designed biochemical assays used in determining IC50 values can be well-suited as surrogates for k.inact/K.i measurements. (

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Are fused tetrahydroquinolines interfering with your assay?

Molecular Design

I’ll be taking a look at B2023 (Fused Tetrahydroquinolines Are Interfering with Your Assay) in this post. The article has already been discussed in posts at Practical Fragments and In The Pipeline. These compounds are found ubiquitously throughout commercial and academic small molecule screening libraries. [

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Unique self-activating proteins for drug discovery

Drug Target Review

Å resolution) 6 is now being targeted for small molecule inhibitor discovery and development, by exploiting emergent computational tools to identify potential candidate compounds in silico and then test these predicted inhibitors in in vitro biochemical assays. NIH R01 DA048153 (to D.P.S.),