Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Sall
D J
DJ
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.
Bastian
J A
JA
Briggs
S L
SL
Buben
J A
JA
Chirgadze
N Y
NY
Clawson
D K
DK
Denney
M L
ML
Giera
D D
DD
Gifford-Moore
D S
DS
Harper
R W
RW
Hauser
K L
KL
Klimkowski
V J
VJ
Kohn
T J
TJ
Lin
H S
HS
McCowan
J R
JR
Palkowitz
A D
AD
Smith
G F
GF
Takeuchi
K
K
Thrasher
K J
KJ
Tinsley
J M
JM
Utterback
B G
BG
Yan
S C
SC
Zhang
M
M
D000818:Animals; D001665:Binding Sites; D018360:Crystallography, X-Ray; D006801:Humans; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors*
D015842:Serine Proteinase Inhibitors; D013876:Thiophenes; C088015:benzothiophene; D013917:Thrombin