Mapping the kinase domain of Janus Kinase 3.
The utilization and impact of parallel synthesis on lead exploration around initial hit oxindole (1) are described. The emergent SAR, analogue design and functional impact will also be detailed.
Adams
Christopher
C
Aventis Pharmaceuticals, 1041 Route 202-206, PO Box 6800, Bridgewater, NJ 08807, USA.
Aldous
David J
DJ
Amendola
Shelley
S
Bamborough
Paul
P
Bright
Colin
C
Crowe
Sarah
S
Eastwood
Paul
P
Fenton
Garry
G
Foster
Martyn
M
Harrison
Trevor K P
TK
King
Sue
S
Lai
Justine
J
Lawrence
Christopher
C
Letallec
Jean-Philippe
JP
McCarthy
Clive
C
Moorcroft
Neil
N
Page
Kenneth
K
Rao
Sudha
S
Redford
Jane
J
Sadiq
Shazia
S
Smith
Keith
K
Souness
John E
JE
Thurairatnam
Sukanthini
S
Vine
Mark
M
Wyman
Barry
B
D000276:Adjuvants, Immunologic / Q000737:chemistry*; D000818:Animals; D001665:Binding Sites; D002455:Cell Division / Q000187:drug effects; D015195:Drug Design; D004487:Edema / Q000188:drug therapy; D004791:Enzyme Inhibitors / Q000737:chemistry; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D007376:Interleukin-2 / Q000494:pharmacology; D053616:Janus Kinase 3; D051379:Mice; D015125:Oxyquinoline / Q000737:chemistry; D010766:Phosphorylation / Q000187:drug effects; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D011505:Protein-Tyrosine Kinases / Q000737:chemistry* / Q000276:immunology* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
D000276:Adjuvants, Immunologic; D004791:Enzyme Inhibitors; D007211:Indoles; D007376:Interleukin-2; D015125:Oxyquinoline; D011505:Protein-Tyrosine Kinases; C507935:Jak3 protein, mouse; D053616:Janus Kinase 3