Kinase Chemistry – Just a year and a half behind the times.


Posted by kinasepro on March 23, 2009

Aveo’s Vegf inhibitor; currently Ph ii in RCC & NSCLC;


Formerly KRN-951 & pM against 1, 2, & 3

5 Responses to “AV-951”

  1. milkshake said

    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.

  2. goldilocks said

    Will this quinoline suffer the same fate as the quinoline of AMG-458?

  3. fromsgc said

    I think that’s exactly his point: Kinse inhibitor field has run out of ideas…

  4. kinasepro said

    You guy’s haven’t been reading the last 60 years of anti-bacterials then I take it?

  5. milkshake said

    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.

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