Table 10: Ligands with potent affinity for ; ligands bound with values <20 nM at this subtype. The structures of these ligands are in the Ph.D. thesis of Clayton (2011) [22].

Cook code

CM-D45 C19H21N3O490.565.530.30.151.650.23
CM-D4434.356.320.70.330.570.92
JYI-04 (C21H23N3O3)28.316NDND0.511.57
PZII-0280.2ND0.2ND0.321.9
PWZ-009A11.341.311.26ND0.842.03
JYI-01 (C19H20N3O3Br)59.215996ND10.62.88
JYI-03 (C21H21N3O3)185.4107NDND0.9543.34
Ro15-45133.32.62.5ND0.263.8
TG-4-292.83.92.72.10.183.9
JYI-11 (C22H22N3O3F3Si)50005000NDND6483.97
QH-II-0770.060.080.05ND0.124
ZG-63A17.321.629.1ND0.654
ZG-2089.711.210.9ND0.384.6
OMB-183.91.23.417330.85
RY-024 C19H19N3O326.926.318.7ND0.45.1
ZG-2347.2522.149.84ND0.35.25
XHE-III-7477105380.422.25.8
JYI-12 (C19H16N3O3F3)9139NDND4.56.8
DM-2391.5ND0.53ND0.146.89
XHE-III-142.6ND101327
TG-4-298.310.26.9ND0.47.61
DM-2156.74ND7.42ND0.2938.28
JYI-13 (C21H16N3O4F3)500063.7NDND168.38
CGS98950.21NDNDNDND9.3
ZG-16811.210.79.2ND0.479.4
PWZ-007A0.110.10.09ND0.210
PZII-0290.34ND0.79ND0.5210
XHE-II-0240.090.180.32140.2411
XHE-II-0028.318133.91.511
BRETAZENIL0.350.640.2ND0.512.7
JYI-19 (C23H23N3O3S)2.176205NDND3412.7
SVO-8-1482586.90.914
SVO-8-301.15.35.32.80.615
WYS10 C14H9F3N2O20.883625.6ND548.715.3
QH-II-090 (CGS-8216)0.050.080.12ND0.2517
PWZ-00710.230.170.120.4417.31

The affinity of compounds at /BzR recombinant subtypes was measured by competition for [3H]flunitrazepam binding to HEK cell membranes expressing human receptors of compositions 132, 232, 332, 432, 532, and 632 [139]. Data represent the average of at least three determinations with a SEM of ±5%. ND: not determined.