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

Archive for October, 2007

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 »


Posted by kinasepro on October 12, 2007

PF-477736 is Pfizers phase 1 Chk1 inhibitor being given in combination with Gemcitabine. They haven’t confirmed the structure yet, but…


It just so happens that 2007/113671 covers the above Chk1 inhibitor in combination with chemotherapy.   It may be the wrong structure, but till proven thus, it’s on the list.  Click for selectivity. Read the rest of this entry »

Posted in Chk1, Pfizer | 7 Comments »

Steal This Document

Posted by kinasepro on October 10, 2007

You may have noticed the Ro5 tab above. Here’s the spreadsheet.

To the best of my knowledge it’s the most complete list of clinical stage kinase inhibitors in existence. There are bound to be errors and omissions though, so while I of course don’t want anything proprietary please send me references and structures as appropriate. I appreciate the help.

Posted in clinical, General Interest | 10 Comments »

Clinical Roundup

Posted by kinasepro on October 9, 2007

Pharmacopoeia – earned a milestone for p38 inhibitor BMS-582949 going ph2.

Incyte – reported on ph2 Jak inhibitor INCB-18424 (?WO/2005/105814, 2B7A) (decent webcast here The short of it: pretty much the same as steroids … no adverse effects at any dose. check in ~8 minutes).

Exelixis – will bundle reports for ph2 XL-880, XL-647, and ph1 XL-184, XL820, and XL-147 at AACR later this month. The Fools think GSK will pick up 880 and I tend to agree.

Ambit talked about a lot at UBS and updates on AC-220 (ph1 FLT3 inhibitor).

Ardea (RDEA)- is preparing to list on the Nasdaq and has RDEA-119 about to hit ph1.

SGX – spins a yarn suggesting that Novartis took a pass on SGX-393. IND for a different compound expected mid ’08. (Webcast on Thursday)

Ariad – knows all about T315I and SGX… Still no structure for AP-24534 though… IND expected end of the year.

S*Bio – has SB-1518 an oral Jak2 (V617F) inhibitor in development: WO/2007/058628, WO/2007/058627

Posted in clinical | 2 Comments »

Read anything good lately?

Posted by kinasepro on October 5, 2007

Got any advice for somebody who wants to know everything there is to know about Kinases in Drug Discovery? Here’s all I’ve got:

  • Two reviews:

Current Signal Transduction 2007, 67-95

Current Medicinal Chemistry 2006, 1735-1748

  • A book: (haven’t read it yet)

Protein Tyrosine Kinases: From Inhibitors to Useful Drugs

  • Some more books: (that look like I should probably want to read them)

Progress in Medicinal Chemistry
Progress in Heterocyclic Chemistry

  • And did I mention I have a reading list on my reading list?

Posted in General Interest | 6 Comments »


Posted by kinasepro on October 4, 2007

Nerviano‘s got CDC7 inhibitors…

And they look something like:


07/110344, 07/096334, 07/071621

Posted in CDC7, Nerviano | Leave a Comment »

One year in…

Posted by kinasepro on October 4, 2007


…and for some peculiar reason people keep on clicking.

Posted in General Interest | 7 Comments »


Posted by kinasepro on October 4, 2007

Among the first to recognize that intellectuals are allowed to use YouTube too…

UC Berkeley makes lectures available free:

Posted in General Interest | Leave a Comment »

Pdb update

Posted by kinasepro on October 2, 2007

2qoq: 1.6A structure of Epha3 & ‘juxtamembrane’ region via SGC: (looks like I missed this series which was released a few months back starting with 2GSF.

This week there’s also:
2P55: Mek w/ Cl-1040 analog via Pfizer

Posted in PDB | Leave a Comment »


Posted by kinasepro on October 2, 2007

So what are they worth?  TotallyMedicinal’s got the low-low.

TY TM for data: mirrored here.

Posted in Approved | Leave a Comment »