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New image-based cellular profiling tool peers deeply into metabolic biology

Broad Institute

The researchers also looked at the tool’s ability to detect changes in cellular phenotypes after exposure to drugs and small molecule compounds. With high-resolution, cell-based profiling techniques, extracting a large amount of data can be done cheaply and efficiently.

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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. 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

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Chemical con artists foil drug discovery

Molecular Design

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.

Drugs 96
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Archbishop Ussher's guide to efficient selection of development candidates

Molecular Design

Nevertheless, those small molecule 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.