Astex’s unpartnered JAK/Aur/Abl Ph1b nib
poster; clinic; PDB: 2W1G & 2W1I
Posted by kinasepro on March 18, 2009
Posted in Astex, Aurora, bcr abl, JAK | Leave a Comment »
Posted by kinasepro on November 28, 2007
GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437
AP-24534 In here? Earlier Ariad had a double bond wiggling around T315I, in WO/2007/133560 & WO/2007/133562 it’s a triple bond.
And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.
Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.
Posted in Ariad, bcr abl, Cyclacel, GSK, Plk1, Rho, Vertex | 4 Comments »
Posted by kinasepro on October 30, 2007
aka nilotinib, AMN-107 is a Novartis‘ follow-on to Gleevec now approved for CML.
Posted in Approved, bcr abl, gleevec, Novartis | 4 Comments »
Posted by kinasepro on September 18, 2007
2QOH; PPY-A bound to Abl via Ariad; Chem Biol Drug Des
2Z60; PPY-A bound to T315I Abl
(compounds from SGX)
2OH4; Benzimidazole bound to VEGF via GSK JP; J Med Chem
2V7A; PHA-739358 bound to T315I mutant of Abl via Nerviano; Cancer Res
Posted in bcr abl, PDB, VEGF | 5 Comments »
Posted by kinasepro on August 9, 2007
The news today is that LS-104 is in Ph1 and now owned by Aegera from Lymphosign who in turn licsensed it from HSC. Their portfolio of patent applications suggests the compound is likely a tyrphostin derivative.
LS104 is a novel small molecule tyrosine kinase inhibitor of therapeutically significant kinases including Jak2 and Bcr-Abl…In contrast to marketed kinase inhibitor drugs, LS104 inhibits its targets in a non-ATP-competitive manner
I don’ t know about you but I needed a history lesson to get a handle on these…
Posted in bcr abl, biotech, JAK | 2 Comments »
Posted by kinasepro on July 13, 2007
Closes a 40M series D that is. Kudos Pros. Some of the more recent thiazole apps like US20070161645 appear to my eye to be the Src/Abl backup brigade.
wt Abl 1.5 nM
T315I 18 nM
So you like pictures?
Posted in bcr abl, biotech, SRC | 2 Comments »
Posted by kinasepro on February 26, 2007
No, not Canada, A? SF, CA – Here, have a sequal to the Prague entry: This is what you’re missing at YawnFest ’07, err I mean: the MMTC:
Wyeth talks Src/Abl: SKI-606 (American Cyanamid: WO/2000/018740)
Roche talks P38: R1487
And a former Abbot guy is talkinig LCK: A-770041
all great compounds and yadda yadda, just having a hard time seeing anything new here.
Posted in Abbott, bcr abl, Lck, p38, Roche, SRC, Wyeth | 4 Comments »
Posted by kinasepro on February 25, 2007
Everyone looking at Abl these days is trying to wiggle their way around T315 and Ariad’s latest go is described in the app: WO/2007/021937 with a series of styrene-purines. They look to be a follow-on series to the earlier purine stuff described elsewhere.
Structures for their two previous SRC/ABL leads: AP23464 and AP23451 were disclosed but afaik AP24534 has not.
Posted in Ariad, bcr abl | Leave a Comment »
Posted by kinasepro on November 24, 2006
At least the PDB gave us something to look at a few days ago. Here’s a super-cool alignment of dasatinib in Abl to VX-680 in an abl mutant.
Posted in Aurora, bcr abl, BMS, Vertex | Leave a Comment »