Chemistry Reference
In-Depth Information
AcHN
N
S
A
CF
3
O
X
Het
NH
2
R
2
N
N
O
N
R
1
B
HN
R
1
R
2
rTRPV1
b
(Cap)
B/P
c
Compd
Het
X
MW
PSA
clog P
HBD
Rot
AMG 517
A
H
H
CH
0.9
430
77
5.1
1
5
0.73
37
B
H
CH
0.6
472
128
2.9
4
8
0.05
O
H
38
B
N
H
H
CH
2.8
519
132
3.6
4
7
0.04
N
39
B H
2
N
0.8
415
146
3.6
5
4
0.11
40
B H
O
N
0.7
473
141
3.6
4
8
0.04
H
41
B
NH
2
CH
3.8
501
154
2.9
6
7
0.07
O
H
a
Physicochemical properties were calculated using Amgen proprietary software (ADAAPT).
75
b
IC
50
values based on inhibition of capsaicin (500 nM) of
45
Ca
21
into rat TRPV1 expressing CHO cells.
c
Study in male Sprague-Dawley rats dosed (i.v.) at 5mg kg
1
solution in DMSO with sampling at 0.5 h.
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