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


Posted by kinasepro on October 12, 2006

& WO2006104915

Hi Glaxo,

You appear to still be committed to your p38 program for which KP is mighty pleased. Think you could you hurry it up a little though please?

The Evolution of a dream:

Looking at the body of matter here it seem like the difluorophenyl is key. Where does it fit? Well, there’s 3 somewhat relevant kinase PDB’s with this functional group: 1H00, 1PYE, 2CHL interestingly all three have the difluorophenyl ring located in the same space but I’ll be darned if I can get a good overlay with the Glaxo compound.

They’ve published a couple of structures from P38: Org. Lett. 2005, 4753 but they look as though they’re from an alternate series which hasn’t seen nearly as much love.


2 Responses to “WO2006104889”

  1. milkshake said

    I think these are knock-off from the Merck(US) p38 leads. I wonder what happened to all these p38 programs – AFAIK, everybody is mreporting sporadic liver tox problems and so far no company went into phase 3 of clinical trials with a p38 alpha, beta inhibitor.

  2. kinasepro said

    There’s a review on what happened to a handful of these P38 programs anyhow:

    Current Opinion in Drug Discovery & Development (2005), 8(4), 421-430

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