Posted by kinasepro on March 28, 2009
Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208
Keeping pace with CP-690550
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Do these nitriles form reversible covalent adducts with the protein?
3FUP would suggest no
No Cys residue in JAK1/JAK2 for -CN? to act a Michael acceptors.
Um, Michael would imply unsaturation. The nitrile/cysteine protease thing is a pretty special case… Kinases just don’t do that.
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
Meh. Call me naive, but I believed Incyte when they said they were cutting edge. Turned out they were just ripping off Pfizer.
It’s not a rip off – its “fast follower”. Do keep up!
Not keeping pace any more – Pfizzzers compound into P3
which the discerning reader knew back in Feb!
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