KinasePro

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

Archive for November, 2008

Motesanib: A little too good.

Posted by kinasepro on November 20, 2008

Looks like this one might be coming off the ph3 list

O=C(NC1=CC=C(C(C)(C)CN2)C2=C1)C3=CC=CN=C3N([H])CC4=CC=NC=C4

Motesanib‘s got “higher early mortality rates

Posted in Amgen, VEGF | 15 Comments »

Banyu’s WEE1 candidate

Posted by kinasepro on November 7, 2008

Polymorph app: WO/2008/133866

Discovery app: WO/2006/126128

wee1

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Posted in Banyu, Merck & Co., Wee1 | 1 Comment »

Rational design…

Posted by kinasepro on November 5, 2008

? ~ F(x) has some thoughts.

Ever since Captopril, I’ve always thought ‘rational design’ to be over-rated and over-sold.  We can do an awful lot without pin-point accuracy, and frankly we don’t have to understand why something is safe and effective to make it so.  Perhaps Ashutosh has tickled a nerve by bringing it up, but I fail to understand why people prefer this fanciful delusion of rational design to the reality of knowledge-based trial and error, but the primary literature is chock full-o-nuts claiming to be a lot smarter then they really are.  But I digress…

On non-oncology indications, of course Fasudil was approved in Japan in 1995 for ‘vascular spasms in the brain’ or some suchness, and is in Ph3 in the US for a few indicationsPfizer and Incyte each have related Jak inhibitors which have looked promising in Ph2 studies.  Otherwise your looking at Rigel’s Ph2 Syk / Flt3 / Vegf inhibitor R-788 also in trials for RA but more likely to be approved for more acute indications, and then there’s always the p38 inhibitors, like Array’s recent ph2, but who knows if and when this target will deliver.

The fact that there was a Kinase-related conference and nobody could rattle that off suggests I’m not posting enough…

Posted in General Interest | 1 Comment »