Well.. maybe this compound will kill it: Polymorphic Forms / WO/2009/098612 & its from Pfizer no less -
Part Axitinib, part Birb, Part SGX… All MW: 700
Thanks for the email PN.
Archive for the ‘p38’ Category
PH-797804
Posted by kinasepro on June 9, 2009
In Ph2 for COPD & it’s an atropisomer…(biochem)
Who wants to guess if its R or S
Process App: 20080177077
Backup: 20080269264
Posted in p38, Pfizer | 6 Comments »
Nilotinib & P38ß
Posted by kinasepro on April 6, 2009
If you’ve got an IC50 comment here or email me: SGC’s got a new pre-release.
p38ß = MAPK11 (not to be confused w/ p38α) 3GP0
Posted in p38, PDB | 1 Comment »
Plethora ‘o’ PDB’s
Posted by kinasepro on October 14, 2008
GSK’s AKT stuff: 3d0e, 3E8D, 3E87, 3E88; J Med Chem, KP
SGX: Jak2 3E64, 3E63, 3E62, BMCL
Shokat: SRC, SRC, SRC, SRC, PI3K-Gamma, PI3K-Gamma
reminds me of OSI-906 or vice versa
Amgen: P38 J Med Chem; 3DT1
Posted in AKT, CDK2, JAK, Lck, p38, PDB, pi3k | Leave a Comment »
Who cares about the Roche p38 inhibitors?
Posted by kinasepro on September 5, 2008
Probably a few less people in PA then a few months ago, eh? But this one’s been getting press recently:
Posted in p38, Roche | Leave a Comment »
ARRY-797 goes to the dentist…
Posted by kinasepro on November 20, 2007
…to evaluate the efficacy of ARRY-797 in the management of postoperative dental pain…
(C(N)=O)CCC3CC3)=O)=C2)OC4=C(C=C(C=C4)F)F)C](http://img201.imageshack.us/img201/7457/arrayil8.jpg)
still no structure disclosed afaik, but likely a cousin of the above.
Posted in Array, p38 | 5 Comments »
PDB Update
Posted by kinasepro on October 16, 2007
2R9S is Jnk3 bound in an unusual fasion to a quinoline inhbitor:(Reminds me a little of Vertex’s 2ok1) (BMCL)
2NPQ is p38 bound to 2 molecules of octyl-glucoside:
Posted in Jnk, p38, PDB | 6 Comments »
VX-702
Posted by kinasepro on September 15, 2007
![FC1=CC=CC(F)=C1N(C(N([H])[H])=O)C2=CC=C(C(N)=O)C(C3=CC=C(F)C=C3F)=N2](http://img72.imageshack.us/img72/8031/vx702fb1.jpg)
Posted in p38, Vertex | 24 Comments »
PDB Update
Posted by kinasepro on August 21, 2007
BMS has a p38 BMCL with a PDB publishing today as well: 2QD9
CC1)C(C2=CNC3=C2C=C(C(N4CC5=CN=C(C6=CC=C(F)C=C6F)N5CC4)=O)C(OC)=N3)=O](http://img237.imageshack.us/img237/7173/bmsza2.jpg)
This one gives a little pespective to SCIO-469 and the related Scripps stuff: WO/2007/082079,
Posted in p38, PDB | Leave a Comment »
GSK and Ranbaxy in the P38 game
Posted by kinasepro on April 5, 2007
Earlier Ranbaxy had WO/2006/082492 and now its: WO/2007/036791. Add to that GSK has 2 oral P38 inhibitors in the clinic but despite some crafty wording of a recent Ranbaxy press release, the current clinical batch wasn’t an Indian invention. It looks as though GSK has shipped finding more backups overseas.
![O=C1C(C2=CC=CC=C2C)=CC3=CN=C(NC4CCN(C(C5=CC=C(F)C=C5)=O)CC4)N=C3N1[C@@H]6CN(C(C)=O)CC6](http://img169.imageshack.us/img169/3785/ranbaxyee3.jpg)
SB681323: Phii: COPD, Neuropathic pain
GW856553: Phii RA; RA; COPD;
CO)N=C2N1C4=CC=C(F)C=C4F](http://img99.imageshack.us/img99/6171/gskcd8.jpg)
One of them is likely from WO/2006/134382 (compound on the left) The other? Not so obvious. There’s a number of GSK p38 applications, but my guess is it hails from the pyrimidopyridone scaffold: Something like: WO/2003/088972 (above) or WO/2006/104915
Posted in GSK, p38 | 4 Comments »
