Practical Fragments

This blog is meant to allow Fragment-based Drug Design Practitioners to get together and discuss NON-CONFIDENTIAL issues regarding fragments.

28 September 2020

Crude reaction screening by crystallography

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Getting from a fragment to something more useful can be time consuming, and frustrating. Often it requires making lots of inactive analogs. ...
21 September 2020

Eighteenth Annual Discovery on Target Meeting

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Last week CHI held Discovery on Target – virtually of course. There were 20 tracks over three days and more than 650 attendees, down from 1...
13 September 2020

Poll: Conferences in the age of COVID-19

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The last fragment-relevant conference of 2020 is happening this week – virtually of course. I attended my first virtual conference last mon...
07 September 2020

From noncovalent to covalent fragment for NSD1

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As evident at the CHI Drug Discovery Chemistry meeting a couple weeks ago, covalent fragment-based lead discovery is becoming increasingly ...
31 August 2020

Fifteenth Annual Fragment-Based Drug Discovery Meeting

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What a strange year for conferences! Everything fragment-related in the first half of the year was canceled or rescheduled. And when it tur...
2 comments:
24 August 2020

SAR by MicroED?

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Of the dozen-plus methods to find and characterize fragments, only two have historically been able to provide detailed binding information:...
17 August 2020

Merge and grow: Fragment-based activators of SOS1

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The RAS family of proteins is implicated in roughly one third of cancers, and as such has been a long-standing target for drug discovery. Ea...
1 comment:
10 August 2020

A fragment library designed for merging: application to PKCζ

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Advancing fragments in the absence of structural information has a reputation for being so challenging that some people do not even attempt ...
03 August 2020

In situ click chemistry on RNA

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In templated or in situ reactions, bonds form between two fragments that are brought together in the context of a larger molecule such as a...
2 comments:
27 July 2020

Flatland: a nice place to be

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The ideal shape of compounds used for biological screens is a subject of vigorous debate, with some arguing that shapely molecules may be ...
11 comments:
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