/home/corante/public_html/pipeline/ en-us derekb.lowe@gmail.com 2012-02-10T08:23:19-05:00 hourly 1 2000-01-01T12:00+00:00 http://pipeline.corante.com/archives/2012/02/10/the_infinitely_active_impurity.php Everyone who's done drug discovery has encountered this situation: you get what looks like a hit in a screening assay, but when you re-check it with fresh material, it turns out to be inactive. So you go back to the... 75448@/home/corante/public_html/pipeline/ Drug Assays 2012-02-10T08:23:19-05:00 http://pipeline.corante.com/archives/2012/02/02/fluorine_nmr_why_not.php Fluorine NMR is underused in chemistry. Well, then again, maybe it's not, but it's one of those thing that just seems like it should have more uses than it does. (Here's a recent bookon the subject). Fluorine is a great... 75424@/home/corante/public_html/pipeline/ Analytical Chemistry 2012-02-02T11:50:37-05:00 http://pipeline.corante.com/archives/2012/01/06/do_we_believe_these_things_or_not.php Some of the discussions that come up here around clinical attrition rates and compound properties prompts me to see how much we can agree on. So, are these propositions controversial, or not? 1. Too many drugs fail in clinical trials.... 75367@/home/corante/public_html/pipeline/ Drug Development 2012-01-06T09:15:16-05:00 http://pipeline.corante.com/archives/2012/01/05/leadoriented_synthesis_what_might_that_be.php A new paper in Angewandte Chemie tries to open another front in relations between academic and drug industry chemists. It's from several authors at GSK-Stevenage, and it proposes something they're calling "Lead-Oriented Synthesis". So what's that? Well, the paper itself... 75365@/home/corante/public_html/pipeline/ Chemical News 2012-01-05T07:20:41-05:00 http://pipeline.corante.com/archives/2011/12/06/riding_to_the_rescue_of_rhodanines.php There's a new paper coming to the defense of rhodanines, a class of compound that has been described as "polluting the scientific literature". Industrial drug discovery people tend to look down on them, but they show up a lot, for... 75312@/home/corante/public_html/pipeline/ Drug Assays 2011-12-06T08:28:58-05:00 http://pipeline.corante.com/archives/2011/11/07/rating_a_massive_pile_of_compounds.php Here's an interesting exercise carried out in the medicinal chemistry departments at J&J. The computational folks took all the molecules in the company's files, and then all the commercially available ones (over five million compounds), minus natural products, which were... 75261@/home/corante/public_html/pipeline/ Drug Assays 2011-11-07T09:08:24-05:00 http://pipeline.corante.com/archives/2011/10/26/francis_collins_speaks.php With all the recent talk about the NIH's translational research efforts, and the controversy about their drug screening efforts, this seems like a good time to note this interview with Francis Collins over at BioCentury TV. (It's currently the lead... 75242@/home/corante/public_html/pipeline/ Academia (vs. Industry) 2011-10-26T09:42:38-05:00 http://pipeline.corante.com/archives/2011/10/21/does_anyone_want_the_nihs_drug_screening_program.php Science is reporting some problems with the NIH's drug screening efforts: A $70-million-a-year program launched 7 years ago at the National Institutes of Health (NIH) to help academic researchers move into industry-style drug discovery may soon be forced to scale... 75236@/home/corante/public_html/pipeline/ Academia (vs. Industry) 2011-10-21T10:42:48-05:00 http://pipeline.corante.com/archives/2011/10/07/different_drug_companies_make_rather_different_compounds.php Now here's a paper, packed to the edges with data, on what kinds of drug candidate compounds different companies produce. The authors assembled their list via the best method available to outsiders: they looked at what compounds are exemplified in... 75215@/home/corante/public_html/pipeline/ Drug Industry History 2011-10-07T09:20:40-05:00 http://pipeline.corante.com/archives/2011/09/14/lillys_open_screening_program_an_update.php I'm still at the RSC/SCI symposium in Cambridge, and a talk yesterday by Marta Pineiro-Nuñez gives me a chance to update this post about Eli Lilly's foray into opening up its screening to outside collaboration. That effort has been working... 75176@/home/corante/public_html/pipeline/ Drug Assays 2011-09-14T05:07:49-05:00 http://pipeline.corante.com/archives/2011/09/07/get_yer_rhodanines_here.php We've talked here before about the structural class known as rhodanines - the phrase "polluting the scientific literature" has been used to describe them, since they rather promiscuously light up a lot of drug target assays, and almost never to... 75166@/home/corante/public_html/pipeline/ Chemical News 2011-09-07T11:16:14-05:00 http://pipeline.corante.com/archives/2011/09/02/how_many_new_drug_targets_arent_even_real.php So, are half the interesting new results in the medical/biology/med-chem literature impossible to reproduce? I linked earlier this year to an informal estimate from venture capitalist Bruce Booth, who said that this was his (and others') experience in the business.... 75160@/home/corante/public_html/pipeline/ Academia (vs. Industry) 2011-09-02T07:05:32-05:00 http://pipeline.corante.com/archives/2011/08/26/kibdelomycin_a_new_antibiotic_in_a_way.php We're going to need new antibiotics. Everyone knows this, and it's not like no one's been trying to do anything about it, either, but. . .we're still going to need more of them than we have. I'm not predicting that... 75154@/home/corante/public_html/pipeline/ Infectious Diseases 2011-08-26T07:32:17-05:00 http://pipeline.corante.com/archives/2011/08/18/is_anyone_doing_the_pfizer_screening_deal.php A couple of years ago, I wrote here about an initiative from Pfizer. They were proposing letting other (smaller) companies screen their compound collection, with rights to be worked out if something interesting turned up. The thing is, I haven't... 75142@/home/corante/public_html/pipeline/ Drug Assays 2011-08-18T10:14:11-05:00 http://pipeline.corante.com/archives/2011/07/27/bait_and_switch_for_type_b_gpcrs.php You hear often about how many marketed drugs target G-protein coupled receptors (GPCRs). And it's true, but not all GPCRs are created equal. There's a family of them (the Class B receptors) that has a number of important drug targets... 75100@/home/corante/public_html/pipeline/ Biological News 2011-07-27T08:33:49-05:00