Table 7: 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

QH-II-0850.080.060.02ND0.08ND
SH-TSC-2 (BCCT)0.030.04190.035ND69.32ND
QH-II-0920.070.030.04ND0.17ND
QH-II-0770.060.080.05ND0.124
YT-II-7695.342.7970.056ND0.04ND
PWZ-007A0.110.10.09ND0.210
XLI-2860.0510.0640.118ND0.684ND
QH-II-090 (CGS-8216)0.050.080.12ND0.2517
PWZ-00710.230.170.12ND0.4417.31
JYI-570.0760.0760.131ND0.036ND
BRETAZENIL0.350.640.2ND0.512.7
PZII-0280.2ND0.2ND0.321.9
QH-II-0750.180.210.25ND1.340
JYI-420.2570.1460.278ND0.256ND
XHE-II-0240.090.180.32140.2411
SH-I-048A0.7740.17230.383ND0.11ND
JYI-5541.39ND0.504ND24.75ND
JYI-472.7592.2820.511ND0.427ND
DM-2391.5ND0.53ND0.146.89
WY-B-150.920.830.5820804.42646
JYI-64 (C17H12N4FBr)0.3051.1110.62ND0.875000
DM-II-90 (C17H12N4BrCl)0.50510.63ND0.375000
QH-1460.49ND0.76ND7.710000
PZII-0290.34ND0.79ND0.5210
WYS19 C26H32N2O4Si NDND0.89NDNDND
XHE-III-06a12151.837
Ro15-17880.80.91.05ND0.6148
MLT-I-701.11.21.1ND40.31000
XHE-III-041.221.12190.4500
FG82050.42.081.16ND1.54227
PWZ-009A11.341.311.26ND0.842.03
alprazolam0.80.591.43ND1.5410000
XLI-34813.5611.171.578ND82.05ND
QH-II-0821.71.81.6ND6.1100
WY-TSC-4 (WYS8)0.0070.991.63ND51.04ND
SPH-1210.141.191.72ND4479
XLi-JY-DMH ANX33.30.581.9ND4.45000
MMB-III-01631.97210740.26211
MMB-III-1631.97210740.26211
XLI-8TC21.5211.012.155ND4.059ND
6-PBC0.491.212.2ND2.391343
YT-III-27132.541.262.35ND103ND
Ro15-45133.32.62.5ND0.263.8
TG-4-292.83.92.72.10.183.9
TG-II-821.62.92.8 ND11000
OMB-183.91.23.417330.85
YT-II6.9320.87123.518ND5.119ND
PS-1-34B C20H17N4BrOND4.1983.928NDNDND
DMCM5.698.294ND1.04134
MSR-I-0326.218.74ND3.374.9
RY-0083.757.24.14ND1.1144.3
XHE-III-491.35.54.238.711.385.1
JYI-60 (C17H11N2OF)3.731.6354.3ND1.75000
FLUNITRAZEPAM2.22.54.5ND2.12000
XLI-31760.2424.054.562ND0.295ND
QH-II-080b33.74.7ND241000
SPH-1650.632.794.85ND10.41150
SH-I-047.36.1365.1ND7.664ND
SVO-8-301.15.35.32.80.615
WY-B-99-14.44.55.582000472000
YT-III-252.5315.7865.691ND0.095ND
BCCE1.24.95.7ND26.82700
MMB-II-9020245.790.2536
TC-YT-II-76101.11.8975.816ND11.99ND
ZK 934234.14.26ND4.51000
RY-06117136.7ND0.331
JYI-54 (C24H15N3O3F4)2.891726.7ND571890
TG-4-298.310.26.9ND0.47.61
MMB-III-1413136.93331.1333
XHE-II-0173.310725817294
SHU-1-194127481484
XHE-III-137.3ND7.18801.6311
DM-2156.74ND7.42ND0.2938.28
ABECARNIL12.415.37.5ND61000
SVO-8-1482586.90.914
XHE-III-240.25ND822210328
SH-I-89S12.788.5628.145ND3.23ND
PWZ-0854.86138.5ND0.5540
XHE-I-09327.18.91107201162
ZG-16811.210.79.2ND0.479.4
ZG69A6.816.39.2ND0.8554.6
ZG-69a (Ro15-1310)6.816.39.2ND0.8554.6
ZG-2347.2522.149.84ND0.35.25
XHE-II-073A (R ENRICHED)5.91110151.18140
RY-067211210ND0.3742
XHE-III-142.6ND101327
YT-III-272295.914.9810.77ND103.3ND
SPH-3825.410.8ND18.53000
ZG-2089.711.210.9ND0.384.6
MLT-II-183.411.711ND22510000
DM-II-33 (C20H13N3O2BrCl3)88.68511.6ND26.25000
JYI-59 (C22H13N3O2F4)1.082.611.82ND11.55000
XHE-II-006b3.7151218971441000
XHE-II-073B (S-ENRICHED)111712332.1269
CM-B44 (ss)3243123794.3485
WYSC1 C16H16N2O21.0945.4412.3ND69.821.2
JYI-4875.5990.6812.78ND31.28ND
XHE-II-0028.318133.91.511
RY-076262713ND0.722
WZ-11319.213.213.4ND11.5300
SH-I-08511.084.86613.75ND0.24ND
CM-E102326142150.5196
TJH-IV-512.3917.414.5ND31610000
YT-III-38146118.2114.63ND3999ND
CM-A871.624.5414.7310004.611000
diazepam142015ND11ND
RY-053492915ND146
YCT-52.211.4616.3ND20010000
RY-09810.122.216.5ND1.68100
PWZ-09611.13616.9ND1.0751.5
XLi223 C22H20BrN3O2148.7181000102000
XHE-I-0657.2171850057500
SH-I-02B29.82131518ND74.05ND
MLT-II-165.0510.4118.4ND26010000
RY-024 C19H19N3O326.926.318.7ND0.45.1
BCCt0.721518.9ND110.85000
LJD-III-15E1.931419ND70.81000
CM-E09b202219550.4569
RY-I-31104519ND61000
SH-I-03014.4211.0419.09ND1.89ND
YT-III-2319.8323.6519.87ND1.105ND
XHE-II-006a4.74.4201876893531
OMB-19224.62033333.540
XHE-III-06b32332029928.6740

Affinity of compounds at /BzR recombinant subtypes was measured by competition for [3H]flunitrazepam or [3H] Ro15-4513 binding to HEK cell membranes expressing human receptors of compositions 132, 232, 332, 432, 532, and 632 [22, 139]. Data represent the average of at least three determinations with a SEM of ±5%. ND: not determined.