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

Archive for the ‘biotech’ Category


Posted by kinasepro on April 26, 2009

Described as a Pfizer PAK4 candidate of indeterminate status.


Read the rest of this entry »

Posted in biotech | 3 Comments »


Posted by kinasepro on April 23, 2009

Some have walked a country mile to get away from the hydroxamate, others think nothing of tacking ‘nother one on:  Its Chugai’s ‘ATP-Collaborative’  Ph1 MEK inhibitor: Ro-4987655 / CH-4987655.  More potent, stable, and soluble…


Reduced signs of hydrolysis to the inactive acid and no BBB penetration.(preclinically)

Posted in biotech, MEK, Roche | Leave a Comment »

GSK’s got C-Met

Posted by kinasepro on March 19, 2009

WO/2008/049855 bears a certain resemblance to XL-184.


btw: XL-880 is now going by GSK-1363089

Posted in biotech, c-Met, GSK | Leave a Comment »

Go Here

Posted by kinasepro on March 4, 2009

It looks good.

pk091 Stefan Knapp will be there with a session entitled: “Strategies for the rational design of selective kinase inhibitors”  I suspect that will be worth the price of admission.

Oh, and why yes that is the same PDB in their flyer that’s been in my header image for the last  while…

Posted in biotech | Leave a Comment »

Palau ‘n’ Jak3

Posted by kinasepro on October 11, 2008

Palau’s got Jak3: WO/2008/119792, purines for Jak3: WO/2008/090181 too.  From the sound of their pipeline DP1’s in there somewhere.


Posted in biotech, JAK | 1 Comment »

A new PI3K PDB

Posted by kinasepro on September 2, 2008

UCB published they’re spin on LY-294002: 3DPD: BMCL

see also: 1E7V

Posted in biotech, PDB, pi3k | Leave a Comment »


Posted by kinasepro on December 7, 2007

Targegen’s got a press release:

Plans to initiate a multi-center clinical trial of TG101348, an internally discovered, oral, potent, and highly selective JAK2 inhibitor in January, 2008

A poster at ASH:

…Dual-Acting JAK2/FLT3 Small Molecule Kinase Inhibitor for the Treatment of AML

and some pyrimidines in WO/2007/053452:


Posted in biotech, clinical, Flt3, JAK | Leave a Comment »

Piper Jaffray

Posted by kinasepro on December 3, 2007

…It’s an investor dog and pony show, and it was last week. Who was there?

Exelixis: George Scangos had this to say on Kinase selectivity:

We get a lot of questions about whether we think that less specific multi-targeted kinase inhibitors are better then more specific kinase inhibitors. I think there is no general answer to that question. Personal view is when your working on the outside of the cell inhibiting a single molecule leads to efficacy, but the efficacy is limited and you can greatly increase the potency by hitting multiple targets at the same time without increasing the toxicity significantly, and I think there is plenty of clinical data now to show that that’s true.

On the other hand when your working downstream inside the cell in the biochemical pathway I think its important to be very specific and so we have a number of other compounds that work downstream within those pathways that are very specific so we tailor the compounds to what we think will optimize balance between efficacy and safety. We have some multi-targeted inhibitors we have some highly selective inhibitors, and we have some that hit a couple of targets.

They keep taunting us with bubble images of XL-880 and XL-184, So here have a guess:


There was also a bit on you should buy XL-647: its ‘More potent’, ‘More safe’ & ‘hits the T790M mutation’

Incyte: /Flexed on the impressive JAK inhibitor results they expect to tell you all about at ASH and beyond.

OSI: Now profitable with Tarceva, whose main competition interestingly enough is Alimta. It sounds like they are keeping OSI-906 for now, but OSI-930 and OSI-632 seem to be for sale.

Infinity: was there dropping some knowledge on the chaperoneness of HSP90 as it relates to kinase inhibitors and resistance.

Posted in biotech, Exelixis, OSI | 2 Comments »

Pfizer’s Jnk

Posted by kinasepro on November 15, 2007

SD’s got a series of Jnk1 inhibitors in WO/2007/125405:


First half of the compounds look about like that one, and Jnk1 data is given…
Second half appear discretely in the claims and look more like Jnk3 inhibitors to me.

Posted in biotech, Jnk, Pfizer | 3 Comments »


Posted by kinasepro on October 27, 2007

Buy this compound?


From: WO/2006/010127 and recently described as inhibiting PKC.

Go ahead, laugh it up – but hey, it could always be worse:

Posted in biotech | 20 Comments »