 |
PDBsum entry 3n4c
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Hydrolase/hydrolase inhibitor
|
PDB id
|
|
|
|
3n4c
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
6-Phenyl-1h-Imidazo[4,5-C]pyridine-4-Carbonitrile as cathepsin s inhibitors.
|
|
|
Authors
|
|
J.Cai,
M.Baugh,
D.Black,
C.Long,
D.Jonathan bennett,
M.Dempster,
X.Fradera,
J.Gillespie,
F.Andrews,
S.Boucharens,
J.Bruin,
K.S.Cameron,
I.Cumming,
W.Hamilton,
P.S.Jones,
A.Kaptein,
E.Kinghorn,
M.Maidment,
I.Martin,
A.Mitchell,
Z.Rankovic,
J.Robinson,
P.Scullion,
J.C.Uitdehaag,
P.Vink,
P.Westwood,
M.Van zeeland,
L.Van berkom,
M.Bastiani,
T.Meulemans.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2010,
20,
4350-4354.
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as
potent and selective cathepsin S inhibitor against both purified enzyme and in
human JY cell based cellular assays. This core has a very stable thio-trapping
nitrile war-head in comparison with the well reported pyrimidine-2-carbonitrile
cysteine cathepsin inhibitors. Compound 47 is also very potent in in vivo mouse
spleenic Lip10 accumulation assays.
|
|
|
|
|
|
|
