RDEA-119

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.

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

PF-3758309

Described as a Pfizer PAK4 candidate of indeterminate status.

AS-703026

>> 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

CH-4987655

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)

MK-2206

Merck‘s Ph1 allosteric AKT inhibitor:

Binds to the Pleckstrin homology domain
@
Akt1 8 nM
Akt2 12 nM
Akt3 65 nM

thanks Ghost and Redferret for the structure

WO/2009/047163

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

Compound A

@ AACR?

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)

CX-4945

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

Ki 0.38 nM

WO/2009/035159

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

for Alzheimer’s & Diabetes

AV-412

Aveo’s Ph1 irreversible  Erbb inhibitor:

via Mitsubishi