INCB018424
Posted by kinasepro on March 28, 2009
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Journals (beta)Posted by kinasepro on March 28, 2009
N2N=CC(C3=NC=NC4=C3C=CN4)=C2](https://kinasepro.files.wordpress.com/2009/03/incb018424.jpg?w=510&h=240 "incb018424")
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Ed said
Do these nitriles form reversible covalent adducts with the protein?
kinasepro said
3FUP would suggest no
OrgMed said
No Cys residue in JAK1/JAK2 for -CN? to act a Michael acceptors.
kinasepro said
Um, Michael would imply unsaturation. The nitrile/cysteine protease thing is a pretty special case… Kinases just don’t do that.
http://pubs.acs.org/doi/abs/10.1021/jm8008597
Ed said
I was thinking more along the lines of the catalytic lysine reacting – but that xray would tend to suggest otherwise – other than the slightly bent CN triple bond
weirdo said
Meh. Call me naive, but I believed Incyte when they said they were cutting edge. Turned out they were just ripping off Pfizer.
Ed said
It’s not a rip off – its “fast follower”. Do keep up!
Ed said
Not keeping pace any more – Pfizzzers compound into P3
http://www.fiercebiotech.com/story/pfizer-moves-ra-pain-drugs-phase-iii/2009-04-02
kinasepro said
which the discerning reader knew back in Feb!