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

More weekend reading…

Posted by kinasepro on November 4, 2007

Reader RGS really wants you to read AZ’s Nature DD article on Ro5 (mostly clogp/mw)

Astex compiled a table for kinase inhibitors.

GMC has a lot to say on the topic.

KP thinks you can skip today’s lesson if you just stop making 600 mw compounds.


5 Responses to “More weekend reading…”

  1. DrSnowboard said

    Call me cheap but not paying $55.10 to read an astex lit review.. I assume it’s not an infomercial.
    Vx-950 mwt 679?
    Anyone else want to fish out some exceptions?

  2. milkshake said

    Ro5 is always ment to be just a mnemonics and shorthand for good drug-desing practices. Management people took it way too seriously.

    But it quite remarkable how unsightly the approved kinase inhibitors are – especially those used for cancer. I guess future kinase drugs for long-term use – in metabolic, neurologic and immune system applications – will look more like traditional drugs (rather than Q-NH-QQQQQ-S, where Q is a nasty-looking heterocycle and S a tertiary-amine sidechain)

  3. kinasepro said

    Your cheap, but its prolly not worth $55.10 when you can get more free.

    I wouldn’t argue that a 600 mw can’t have oral availability and go on to be a successful drug, only that its less likely to do so!

    Whether it’s to sell the value of your compounds to your boss during year end performance review time, a potential partner during diligence time, or a potential clinicians at ph1 time. Ro5 compounds are just going to be more valuable.

    btw, your example might even prove the point, given some recent events that suggest Telaprevir (VX-950; mw 679) might just get its ass kicked by Boceprevir (SCH-503034; mw 520).

  4. DrSnowboard said

    True Vertex have a battle on their hands, but they do have a very professional / slick science-marketing attitude – StatC anyone?. Dosing frequency and side-effect incidence is going to hurt at some point, but then doesn’t it always for first-in-class that makes it to market?

  5. Sometimes I feel that the one thing I get from all these discussions- lots of ugly molecules being pursued inspite of their unseemly architecture- is that pharma companies are in big trouble…

    The second thing I get is “the only think I know is that I know nothing” by Socrates.

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