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

Archive for April, 2009


Posted by kinasepro on April 29, 2009

Its Ardeas’s $35 million non-hydroxamate MEK inhibitor in Ph1.  The pictured structure is one of three claimed in the ‘combination w/ Nexavar’ app: WO/2009/018238.

rdeaArdea will grant Bayer a worldwide, exclusive license to develop and commercialize Ardea’s MEK inhibitors for all indications”

Posted in Bayer, MEK | 1 Comment »


Posted by kinasepro on April 26, 2009

Described as a Pfizer PAK4 candidate of indeterminate status.


Read the rest of this entry »

Posted in biotech | 3 Comments »


Posted by kinasepro on April 24, 2009

>> Update – this structure has been revised from the butyl amide – This is (i believe) the correct structure >>

EMD-Serono’s got ‘a ph1 non-hydroxamate ‘ATP Collaborative’ Mek inhibitor.


via Ghost, & WO/2006/045514

Posted in MEK, Merck DE | 5 Comments »


Posted by kinasepro on April 23, 2009

Some have walked a country mile to get away from the hydroxamate, others think nothing of tacking ‘nother one on:  Its Chugai’s ‘ATP-Collaborative’  Ph1 MEK inhibitor: Ro-4987655 / CH-4987655.  More potent, stable, and soluble…


Reduced signs of hydrolysis to the inactive acid and no BBB penetration.(preclinically)

Posted in biotech, MEK, Roche | Leave a Comment »


Posted by kinasepro on April 23, 2009

Merck‘s Ph1 allosteric AKT inhibitor:

NC1(CCC1)C(C=C2)=CC=C2C3=NC4=C(C=C3C5=CC=CC=C5)C(N6C=C4)=NNC6=OBinds to the Pleckstrin homology domain
Akt1 8 nM
Akt2 12 nM
Akt3 65 nM

thanks Ghost and Redferret for the structure

Posted in AKT, Merck | 6 Comments »


Posted by kinasepro on April 22, 2009

WO/2009/047163 show’s a series of minimalist designed CK1 inhibitors:


Compound A


Posted in CK1, Roche | 2 Comments »


Posted by kinasepro on April 19, 2009

Send Structures / Will Post!

Email me smiles/inchi/chemdraw/iupac – whatever.  Structure and a corporate number is good enough, but any other info – feel free. (please include whether you want to be anon)

Posted in General Interest | Leave a Comment »


Posted by kinasepro on April 19, 2009

Cylene’s CK2-α selective inhibitor currently in Ph1:


Ki 0.38 nM

Posted in CK2 | 9 Comments »


Posted by kinasepro on April 13, 2009

Possibly SAR-502250 its a Mitsubishi / Sanofi TPK1/GSK3 inhibitor:


for Alzheimer’s & Diabetes

Posted in GSK3, Sanofi-Aventis | 2 Comments »


Posted by kinasepro on April 13, 2009

Aveo’s Ph1 irreversible  Erbb inhibitor:


via Mitsubishi

Posted in EGF | 2 Comments »