 |
PDBsum entry 2waj
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
1-Aryl-3,4-Dihydroisoquinoline inhibitors of jnk3.
|
|
|
Authors
|
|
J.A.Christopher,
F.L.Atkinson,
B.D.Bax,
M.J.Brown,
A.C.Champigny,
T.T.Chuang,
E.J.Jones,
J.E.Mosley,
J.R.Musgrave.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2009,
19,
2230-2234.
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
A series of 1-aryl-3,4-dihydroisoquinoline inhibitors of JNK3 are described.
Compounds 20 and 24 are the most potent inhibitors (pIC50 7.3 and 6.9,
respectively in a radiometric filter binding assay), with 10- and 1000-fold
selectivity over JNK2 and JNK1, respectively, and selectivity within the wider
mitogen-activated protein kinase (MAPK) family against p38alpha and ERK2. X-ray
crystallography of 16 reveals a highly unusual binding mode where an H-bond
acceptor interaction with the hinge region is made by a chloro substituent.
|
|
|
|
|
|
|
