31 December 2019

Review of 2019 reviews

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The year ends, and with it the awkward teenage phase of the twenty-first century. As we have done since 2012 , we're using this last p...
3 comments:
16 December 2019

Fragments in the clinic: S64315 / MIK665

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Earlier this year we highlighted the discovery of AZD5991, a phase 1 compound from AstraZeneca that inhibits the anti-apoptotic cancer tar...
09 December 2019

A new library of fluorinated Fsp3-rich fragments

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Among fragment-finding methods , ligand-based NMR ranks near the top in terms of popularity. Of its many variations, fluorine ( 19 F) NMR...
2 comments:
02 December 2019

Poll results: affiliation and fragment-finding methods in 2019

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The fourth iteration of our fragment-finding methods poll has just closed. If you want to jump right to the results feel free to skip the ...
2 comments:
25 November 2019

Reverse micelle encapsulation for measuring low affinities

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NMR is among the more sensitive fragment-finding techniques: the starting point for clinical compound ASTX660 had low millimolar affinity ...
18 November 2019

Fragment-based Drug Design Down Under 2019

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The last major fragment meeting of 2019 took place at the Monash Institute of Pharmaceutical Sciences, Monash University, in marvelous Mel...
10 November 2019

A new tool for detecting aggregation

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Historically the most popular method for finding fragments has been ligand-detected NMR. Preliminary results of our current poll (to the r...
1 comment:
04 November 2019

Second harmonic generation (SHG) vs KRAS

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Practical Fragments is currently running a poll on fragment-finding methods used by readers – please vote on the right-hand side. One biop...
2 comments:
20 October 2019

New poll: affiliations and methods

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It has been three years since we last asked about fragment-finding methods, and a lot can change in that time – just compare the world tod...
14 October 2019

Fragments vs Mycobacterium TrmD – and native ESI-MS revisited

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The Mycobacterium genus of bacteria contains more than 190 species, including the pathogens that cause leprosy and tuberculosis. Mycobacte...
07 October 2019

The story of erdafitinib – abridged

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In April we celebrated the FDA approval of erdafitinib for certain types of urothelial carcinomas with genetic alterations in the FGFR2 or...
30 September 2019

Combining fragments and HTS hits to target PHGDH

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Boehringer Ingelheim has been on something of a tear reporting new chemical probes for difficult targets – see here for their NSD3 inhibi...
23 September 2019

Seventeenth Annual Discovery on Target

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Just as April brings CHI’s Drug Discovery Chemistry in San Diego, September brings CHI’s Discovery on Target in Boston, and last week saw...
16 September 2019

Fragments find flexibility in fascin 1

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Protein flexibility can be both an opportunity and a barrier – quite literally, when a solid wall of protein seems to block opportunities ...
09 September 2019

Fragments vs sepiapterin reductase, via 19F NMR

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It has been two years since we’ve had a post devoted to fluorine NMR. Though I don't share Teddy’s “ fetish ” for 19 F-based screening...
02 September 2019

Fragment vs hematopoietic prostaglandin D2 synthase: a chemical probe

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Six years ago we highlighted work out of GlaxoSmithKline and Astex describing some of their efforts to find inhibitors of hematopoietic pr...