This entry was posted on March 23, 2009 at 12:18 am and is filed under VEGF.
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You know, these kinase ligand structures you listed here, stacked on the same page, they all look pretty terrible from the design point of view. I might start on a non-kinase CNS receptor target in the near future and I can’t wait.
antibiotic structures are truly baroque but antibiotics don’t have to get into a cell.
No I don’t think kinase field has run out of ideas – and besides, what we see published is often few years behind the curve – its just that kinase binding sites naturally love poly-heteroaromatic ligands that are flat and long, like bunch of beads on a string, and have lots of NH groups, carbonyls and heterocyclic nitrogens, (plus some kind of amine appendage to make that thing soluble) and putting biaryls together by Suzuki and diaryl amines/ethers by Buchwald is a rather favorite medchem thing to do.