/home/corante/public_html/pipeline/ en-us derekb.lowe@gmail.com 2013-06-17T07:55:54-05:00 hourly 1 2000-01-01T12:00+00:00 http://pipeline.corante.com/archives/2013/06/17/aggravating_aggregators.php Compound aggregation is a well-known problem in biochemical assays (although if you go back a few years, that certainly wasn't the case). Some small molecules will start to bunch up under some assay conditions, and instead of your target protein... 76482@/home/corante/public_html/pipeline/ Drug Assays 2013-06-17T07:55:54-05:00 http://pipeline.corante.com/archives/2013/06/07/making_peroxides_quietly_and_unhelpfully.php Here's a problem with screening collections that I have to admit I wasn't aware of: generation of hydrogen peroxide. This paper (free access) gives an excellent overview of what's going on. Turns out that some compounds can undergo redox-cycling in... 76463@/home/corante/public_html/pipeline/ Drug Assays 2013-06-07T06:43:20-05:00 http://pipeline.corante.com/archives/2013/05/15/gsks_published_kinase_inhibitor_set.php Speaking about open-source drug discovery (such as it is) and sharing of data sets (such as they are), I really should mention a significant example in this area: the GSK Published Kinase Inhibitor Set. (It was mentioned in the comments... 76417@/home/corante/public_html/pipeline/ Academia (vs. Industry) 2013-05-15T06:28:27-05:00 http://pipeline.corante.com/archives/2013/05/10/why_not_share_more_bioactivity_data.php The ChEMBL database of compounds has been including bioactivity data for some time, and the next version of it is slated to have even more. There are a lot of numbers out in the open literature that can be collected,... 76407@/home/corante/public_html/pipeline/ Drug Assays 2013-05-10T06:46:54-05:00 http://pipeline.corante.com/archives/2013/05/03/drug_assay_numbers_all_over_the_place.php There's a truly disturbing paper out in PLoSONE with potential implications for a lot of assay data out there in the literature. The authors are looking at the results of biochemical assays as a function of how the compounds are... 76387@/home/corante/public_html/pipeline/ Drug Assays 2013-05-03T06:11:58-05:00 http://pipeline.corante.com/archives/2013/04/16/whats_translational_synthesis_anyway.php There's another paper in the Nature Chemical Biology special issue that I wanted to mention, this one on "Translational Synthetic Chemistry". I can't say that I like the title, which seems to me to have a problem with reification (the... 76346@/home/corante/public_html/pipeline/ Drug Assays 2013-04-16T22:05:24-05:00 http://pipeline.corante.com/archives/2013/04/11/fragments_for_receptors_it_can_be_done.php The advent of real X-ray structures for receptors means that there are many experimental approaches that can now be tried that earlier would have been (most likely) foolhardy. My first research in the industry was on dopamine receptors, which I... 76340@/home/corante/public_html/pipeline/ Drug Assays 2013-04-11T09:19:12-05:00 http://pipeline.corante.com/archives/2013/04/10/pharmacology_versus_biology.php There's a comment made by CellBio to the recent post on phenotypic screening that I wanted to highlight I think it's an important point: In drug discovery, we need fewer biologists dedicated to their biology, and more pharmacologists dedicated to... 76338@/home/corante/public_html/pipeline/ Drug Assays 2013-04-10T09:23:01-05:00 http://pipeline.corante.com/archives/2013/04/09/mass_spec_continues_its_conquests.php You know, mass spectrometry has been gradually taking over the world. Well, maybe not your world, but mine (and that of a lot of biopharma/biophysical researchers). There are just so many things that you can do with modern instrumentation that... 76335@/home/corante/public_html/pipeline/ Analytical Chemistry 2013-04-09T07:08:43-05:00 http://pipeline.corante.com/archives/2013/04/08/the_basics_of_phenotypic_screening.php I wanted to mention another paper from Nature Chemical Biology's recent special issue, this one on the best ways to run phenotypic screens. This area has been making a comeback in recent years (as discussed around here before), so articles... 76330@/home/corante/public_html/pipeline/ Drug Assays 2013-04-08T06:47:06-05:00 http://pipeline.corante.com/archives/2013/04/04/good_ways_to_mess_up_your_screening.php For those of you interested in fragment screening (and especially for those who are thinking of trying it out), Ben Davis of Vernalis and Dan Erlanson of Carmot Therapeutics have written an excellent guide to avoiding the common experimental problems.... 76324@/home/corante/public_html/pipeline/ Drug Assays 2013-04-04T06:39:25-05:00 http://pipeline.corante.com/archives/2013/03/27/the_dnaencoded_library_platform_yields_a_hit.php I wrote here about DNA-barcoding of huge (massively, crazily huge) combichem libraries, a technology that apparently works, although one can think of a lot of reasons why it shouldn't. This is something that GlaxoSmithKline bought by acquiring Praecis some years... 76307@/home/corante/public_html/pipeline/ Chemical Biology 2013-03-27T10:47:18-05:00 http://pipeline.corante.com/archives/2013/03/26/automated_medchem_at_last.php I've written several times about flow chemistry here, and a new paper in J. Med. Chem. prompts me to return to the subject. This, though, is the next stage in flow chemistry - more like flow med-chem: Here, we report... 76305@/home/corante/public_html/pipeline/ Chemical News 2013-03-26T10:43:03-05:00 http://pipeline.corante.com/archives/2013/03/13/getting_down_to_proteinprotein_compounds.php Late last year I wrote about a paper that suggested that some "stapled peptides" might not work as well as advertised. I've been meaning to link to this C&E News article on the whole controversy - it's a fine overview... 76274@/home/corante/public_html/pipeline/ Drug Development 2013-03-13T06:37:12-05:00 http://pipeline.corante.com/archives/2013/03/04/putting_the_hard_chemistry_back_in_med_chem.php While I'm on the subject of editorials, Takashi Tsukamoto of Johns Hopkins has one out in ACS Medicinal Chemistry Letters. Part of it is a follow-up to my own trumpet call in the journal last year (check the top of... 76251@/home/corante/public_html/pipeline/ Drug Industry History 2013-03-04T09:45:18-05:00