A novel series of potent and selective IKK2 inhibitors.
A novel series of aminopyrimidine IKK2 inhibitors have been developed which show excellent in vitro inhibition of this enzyme and good selectivity over the IKK1 isoform. The relative potency and selectivity of these compounds has been rationalized using QSAR and structure-based modelling.
Bingham
Alistair H
AH
Celltech R&D Ltd, Granta Park, Great Abington, CB16GS, Cambridge, UK.
Davenport
Richard J
RJ
Gowers
Lewis
L
Knight
Roland L
RL
Lowe
Christopher
C
Owen
David A
DA
Parry
David M
DM
Pitt
Will R
WR
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051550:I-kappa B Kinase; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology
D004791:Enzyme Inhibitors; D011743:Pyrimidines; D017346:Protein Serine-Threonine Kinases; D051550:I-kappa B Kinase