KinasePro

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

INCB018424

Posted by kinasepro on March 28, 2009

Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208

N#CC[C@H](C1CCCC1)N2N=CC(C3=NC=NC4=C3C=CN4)=C2

Keeping pace with CP-690550

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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

    http://www.fiercebiotech.com/story/pfizer-moves-ra-pain-drugs-phase-iii/2009-04-02

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