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

Archive for October 4th, 2006


Posted by kinasepro on October 4, 2006

Hello Crazy Germans, errr I mean Hi Merck KGaA.

While everyone else is making pyrimidines, quinazolines, and assorted one or two-offs here comes Merck with umm this:?

I guess they look a little like the CDK compounds from J. Med. Chem. 2006, 44, 4628, but not really.

Kinaspro’s German isn’t all that good, but it looks as though they too speak Kinese:

Posted in Merck DE, PDGFR, TIE2, VEGF | Leave a Comment »


Posted by kinasepro on October 4, 2006

Hi TargeGen, Kinasepro cares less about who you are (and who are you, btw?) and more about whatchagot. Don’t let’m tell you you’ve just got another VEGF inhibitor, because Kinasepro likes your application. Why does Kinasepro like your application? Because you give data. While others scoff and claim all compounds <10 uM you proudly boast your yes/src/vegf/ephb4/fgf profile! Good show. Now if you could just figure out how to sell it…

While everyone’s seen the few zillion 2,4 diamopyrimidines that seem to crop up again and again (for that matter, has anyone figured out why JACS, 2006, 2182 is a JACS?) The focus here on 2,5 adds a little zest to the mix and proves there’s more then one way into H1. Seems like there’s something special about the chlorophenol. ** Kinasepro wonders aloud about the isosteric indole.


In fact the only guys I’ve seen that used the 2,5-pyrimidine motif published: BMCL, 2006, 1320 (PDB 2C6E) and that binding strategy’s gotta be different. Ummm right?

>> Update >> With a new BMCL, data in the patent, and multiple talks at the last ACS meeting all fingers point to a SRC/Yes/EphB4 fire sale! Got a spare million?

Posted in biotech, SRC, VEGF | Leave a Comment »


Posted by kinasepro on October 4, 2006

Hi BMS, Yet another EGF inhibiting Quinazoline series, I see?

I had the good fortune to work with Ping Chen a few thousand years ago, in a galaxy far far away. Ping (a coinventor on this patent) is one of those brilliant BMS ‘Schlessinger Guys’ with a work ethic of a pack mule. I mean, how many industry guys do you know that are taking NMR’s at 8 O’clock every night?

Looks as though they’re sticking a piperidine in the ribose pocket.

I like it, but I’m surprised that I don’t recall seeing someone pull this off before.


Overlays nicely in Pymol to 2GS7 using 1XKK for the alignment.

example overlay

Posted in BMS, EGF | 2 Comments »