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The researchers also looked at the tool’s ability to detect changes in cellular phenotypes after exposure to drugs and smallmolecule compounds. With high-resolution, cell-based profiling techniques, extracting a large amount of data can be done cheaply and efficiently.
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. Subscripting doesn't work well in blogger and so I'll use K.i I’ll start with Section 2.1 As measurement of k.inact/K.i
My main criticism of BW2014 that is that the rhetoric is not supported by data and I’ve always seen the article as something of a propaganda piece. I was rather surprised that BW2014 had not cited a single article about how colloidal aggregation can foil drug discovery. Given that M2003 had been published over a decade previously.
Nevertheless, those smallmolecule drug properties that show consistent differentiation from their target compounds over time, namely, potency, ligand efficiencies (LE and LLE), and the aromatic ring count and lipophilicity of carboaromatic drugs, are those that are most likely to remain future-proof.
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