Chemistry Reference
In-Depth Information
NMe
2
X
O
44-58
Y
SRI IC
50
(nM)
a
Selectivity over
DRI
Selectivity over
NRI
Compound
Y
X
clog P
log D
44 OCF
3
NHSO
2
Me 14 2028 565 3.9 -
45 OCF
3
CONH
2
3 12 387 1394 3.6 2.3
46 OCF
3
CONHMe 10 1441 275 3.8 -
47 OCF
3
SO
2
NH
2
9 920 6283 3.3 2.2
48 OCF
3
SO
2
NHMe 11 2056 444 3.9 -
49 OCF
3
CH
2
NHSO
2
Me 11 530 520 3.8 2.1
50 CF
3
NHSO
2
Me 5 2375 166 3.8 2.3
51 CF
3
CONH
2
9 2217 109 3.5 -
52 CF
3
CONHMe 11 1523 114 3.7 -
53 CF
3
CONMe
2
39 698 11 3.4 -
54 CF
3
SO
2
NHMe 9 265 265 3.7 -
55 CF
3
SO
2
NMe
2
79 164 38 4.2 -
56 CF
3
CH
2
OH 13 40 95 3.9 -
57 CF
3
CH
2
NH
2
59 43 236 3.9 -
58 CF
3
CH
2
NHSO
2
Me 55 49 62 3.6 -
a
The inhibitory potency at human serotonin, dopamine and noradrenaline transporters was quantified through measurement of a compound's ability to inhibit
transport and subsequent intracellular accumulation of radiolabelled ligand in an in vitro radiometric assay using HEK-293 cells stably expressing the appropriate
transporters. All assay determinations are Zn
ΒΌ
2.
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