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

Archive for the ‘bcr abl’ Category


Posted by kinasepro on March 18, 2009

Astex’s unpartnered JAK/Aur/Abl Ph1b nibO=C(NC1=CNN=C1C2=NC3=C(N2)C=CC(CN4CCOCC4)=C3)NC5CC5

poster; clinic; PDB: 2W1G & 2W1I

Posted in Astex, Aurora, bcr abl, JAK | Leave a Comment »

Some highlights…

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 »

Tasigna Approved

Posted by kinasepro on October 30, 2007

aka nilotinib, AMN-107 is a Novartis‘ follow-on to Gleevec now approved for CML.


wiki; clinic; WO/2002/022597

Posted in Approved, bcr abl, gleevec, Novartis | 4 Comments »

PDB Update

Posted by kinasepro on September 18, 2007

Big week

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

2IN6 Wee1
2IO6 Wee1

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 »

TargaGen closes…

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?

Read the rest of this entry »

Posted in bcr abl, biotech, SRC | 2 Comments »

Who’s in CA?

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 »

AP24534 In here?

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 January 5, 2007

Making some bold claims, Innovive gets orphan status for INNO-406 / NS-187



Posted in bcr abl, clinical, lyn | 3 Comments »

BMS-354825 vs. VX-680

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 »