EXEL & CK2

And then theres those 3 applications on CK2 from Exelixis WO/2007/048064, WO/2007/048065, & WO/2007/048066… The latter two with and / or Pim1 & 2 inhibition.

Seems plausible that CK2 could be one of the ‘undisclosed’ targets of the BMS collaboration.

ARQ-197

Hard to spit in the sink at ‘30 million for the Asian rights‘ to a ph1 compound…

WO/2006/086484

The Thursday List

US20070093537 p38 BMS
US20070093532 Raf Merck DE
US20070093516 Lyn
US20070093513 Rho Senju
US20070093512 egf GSK
US20070093506 Novartis
US20070093491 ?
US20070093446
US20070093480 IGF1R+ Sanofi Aventis
US20070093488 Aurora/CDK Sanofi Aventis
US20070093490 PCK / Alk
WO/2007/046426 ATR NIIGATA
WO/2007/047646 Aurora Janssen
WO/2007/048064 CK2 Exelixis
WO/2007/048065 CK2 Exelixis
WO/2007/048066 CK2 Exelixis
WO/2007/048070 Amgen
WO/2007/048088 Flt3 Janssen

XL-765

mTOR / Pi3k inhibitor IND application reported today. XL-147 is their other one, and three pi3k applications published last Thursday. WO/2007/044698, WO/2007/044729, WO/2007/044813

Till Nature disables hotlinking: here’s who’s got what from here.

PDB Update

>> Update >> Biochemistry article on the Plk1 structure.

Woohoo! First published kinase domain Plk1 structures from Pfizer:

2OWB Plk1 w/ pyrrolopyrazole inhibitor
2OU7 Plk1 w/ ANP

and a Chk1 structure from Merck: 2HOG; BMCL

Takeda w/ more-a Aurora

Takeda has been looking at compounds similar to vx-680 for a while now, and the same group now has WO/2007/044779. The pretty colors give an idea whats going on, but frankly we all suck at drawing squishy things… for now your stuck with pymol!

2BFY shows a sulfonamide down thereabout in Aurora-B.

XL-518

My guess is XL-518 is in WO/2007/044515.

362 examples, 15 inventors.

IND beating first app is unusual. kudos.

The Thursday List

This here’s gonna make for a busy weekend.

US20070087393 ZAP-70 Assay…
US20070088019 Gsk3 &/or PKC J&J
US20070088031 Gsk3 GSK
US20070088033 p38 Pharmacia
US20070088037 TGFb Pfizer
US20070088041 Gsk3 Sanofi-aventis
US20070088044 EGFR AstraZeneca
US20070088051 Boehringer Ingelheim
US20070088080 Gsk3 Neuropharma

WO/2007/042298 Syk GSK
WO/2007/042299 Syk GSK
WO/2007/042321 AGC Devgen
WO/2007/042784 Cyclacel
WO/2007/042786 Cyclacel
WO/2007/042806 LIFCR +
WO/2007/042810 Astellas +
WO/2007/044050 IKK BMS
WO/2007/044084 Mek Array
WO/2007/044401 CDK Schering
WO/2007/044407 Schering
WO/2007/044410 Schering
WO/2007/044420 CDK Schering
WO/2007/044426 Schering
WO/2007/044441 Schering
WO/2007/044449 Schering
WO/2007/044515 Mek Exelixis
WO/2007/044698 PI3Kα Exelixis
WO/2007/044724 Pim1 Exelixis
WO/2007/044729 PI3K Exelixis
WO/2007/044779 Takeda
WO/2007/044813 PI3Kα Exelixis
WO/2007/044932 Methods… ActiveSite

Kinase PDBs

Here’s an interestingly derived big list of kinase structures in the PDB. I guess the answer is 112.

PX-866

PX-866 is a Wortmannin analog that came to Biomira as part of the Prolx deal.

You synthetic junkies should recognize at least one of the names on the patent app. Appears to be a simple improvement to the michael acceptor.

1E7U shows the natural product covalently bound to Pi3k