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


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

9 Responses to “INCB018424”

  1. Ed said

    Do these nitriles form reversible covalent adducts with the protein?

  2. OrgMed said

    No Cys residue in JAK1/JAK2 for -CN? to act a Michael acceptors.

  3. 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

  4. 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.

  5. Ed said

    It’s not a rip off – its “fast follower”. Do keep up!

  6. Ed said

    Not keeping pace any more – Pfizzzers compound into P3

Leave a Reply

Fill in your details below or click an icon to log in: Logo

You are commenting using your account. Log Out /  Change )

Google photo

You are commenting using your Google account. Log Out /  Change )

Twitter picture

You are commenting using your Twitter account. Log Out /  Change )

Facebook photo

You are commenting using your Facebook account. Log Out /  Change )

Connecting to %s

%d bloggers like this: