Table 6: Ligands with potent affinity for 2; 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-0920.070.030.04ND0.17ND
SH-TSC-2 (BCCT)0.030.04190.035ND69.32ND
QH-II-0850.080.060.02ND0.08ND
XLI-2860.0510.0640.118ND0.684ND
JYI-570.0760.0760.131ND0.036ND
QH-II-090 (CGS-8216)0.050.080.12ND0.2517
QH-II-0770.060.080.05ND0.124
PWZ-007A0.110.10.09ND0.210
JYI-420.2570.1460.278ND0.256ND
PWZ-00710.230.170.12ND0.4417.31
SH-I-048A0.7740.17230.383ND0.11ND
XHE-II-0240.090.180.32140.2411
QH-II-0750.180.210.25ND1.340
XLi-JY-DMH ANX33.30.581.9ND4.45000
alprazolam0.80.591.43ND1.5410000
YT-50.4210.603436.06ND1.695ND
BRETAZENIL0.350.640.2ND0.512.7
XLi268 C17H13BrN42.81450.6862NDND0.6243ND
WY-B-150.920.830.5820804.42646
YT-II6.9320.87123.518ND5.119
Ro15-17880.80.91.05ND0.6148
XLi351 C21H21ClN2OSi1.5070.967NDND1.985ND
WY-TSC-4 (WYS8)0.0070.991.63ND51.04ND
XLi352 C18H13ClN2O1.560.991NDND1.957ND
DM-II-90 (C17H12N4BrCl)0.50510.63ND0.375000
JYI-64 (C17H12N4FBr)0.3051.1110.62ND0.875000
XLi350 C17H11ClN2O1.2241.188NDND2.9ND
SPH-1210.141.191.72ND4479
MLT-I-701.11.21.1ND40.31000
OMB-183.91.23.417330.85
6-PBC0.491.212.2ND2.391343
YT-III-27132.541.262.35ND103ND
PWZ-009A11.341.311.26ND0.842.03
DM-II-72 (C15H10N20BrCl)50001.37NDND2.025000
JYI-60 (C17H11N2OF)3.731.6354.3ND1.75000
XLI-2TC3.4421.67344.08ND1.121ND
QH-II-0821.71.81.6ND6.1100
TC-YT-II-76101.11.8975.816ND11.99ND
MMB-III-01631.97210740.26211
MMB-III-1631.97210740.26211
XHE-III-06a12151.837
XHE-III-041.221.12190.4500
WYS15 C22H20N2O23.632.0244.3ND76.55000
FG82050.42.081.16ND1.54227
JYI-70 (C19H13N4F)6.32.1NDND0.565000
JYI-472.7592.2820.511ND0.427ND
JYI-49 (C20H12N3O2F4Br)1.872.38NDND6.73390
FLUNITRAZEPAM2.22.54.5ND2.12000
JYI-59 (C22H13N3O2F4)1.082.611.82ND11.55000
Ro15-45133.32.62.5ND0.263.8
SPH-1650.632.794.85ND10.41150
YT-II-7695.342.7970.056ND0.04ND
TG-II-821.62.92.8ND11000
QH-II-080b33.74.7ND241000
TG-4-292.83.92.72.10.183.9
PS-1-34B C20H17N4BrOND4.1983.928NDNDND
ZK 934234.14.26ND4.51000
XHE-II-006a4.74.4201876893531
WY-B-99-14.44.55.582000472000
CM-A871.624.5414.7310004.611000
OMB-19224.62033333.540
SH-I-08511.084.86613.75ND0.24ND
BCCE1.24.95.7ND26.82700
JYI-32 (C20H15N3O2BrF)3.074.96NDND2.9252.24
XHE-I-0387.3534ND1321000
SVO-8-301.15.35.32.80.615
SPH-3825.410.8ND18.53000
WYSC1 C16H16N2O21.0945.4412.3ND69.821.2
JYI-06 (C23H23N3O4)16.55.485000ND12.65000
XHE-III-491.35.54.238.711.385.1
YT-III-252.5315.7865.691ND0.095ND
SH-I-047.36.1365.1ND7.664ND
XHE-I-09327.18.91107201162
RY-0083.757.24.14ND1.1144.3
DMH-D-053 (C43H30N6O4)2367.42725000194.25000
WY-B-09-13.9983210004612000
HJ-I-03715.078.12728.29ND0.818ND
DMCM5.698.294ND1.04134
SH-I-89S12.788.5628.145ND3.23ND
XLi223 C22H20BrN3O2148.7181000102000
CM-A82a2.788.9324.5110007.491000
QH-II-0639.49.331ND7.73000
9.49.331ND7.73000
XHE-II-0173.310725817294
TG-4-298.310.26.9ND0.47.61
MLT-II-165.0510.4118.4ND26010000
JC184 C13H9BrN2OS9.60610.5NDND6.709ND
ZG-16811.210.79.2ND0.479.4
XHE-II-073A (R ENRICHED)5.91110151.18140
XLI-8TC21.5211.012.155ND4.059ND
SH-I-03014.4211.0419.09ND1.89ND
XLI-34813.5611.171.578ND82.05ND
ZG-2089.711.210.9ND0.384.6
YT-TC-3141.411.43118.1ND29.22ND
YCT-52.211.4616.3ND20010000
MLT-II-183.411.711ND22510000
XHE-II-O53-ACID50.3511.844ND5.95000
SHU-1-194127481484
RY-067211210ND0.3742
DM-III-01 (C18H12N3O2Br)500012NDND4.735000
MLT-II-183.912.224.4ND21010000
SH-053-2′F 21.9912.3434.9ND0.671ND
WYS13 C20H18N2O32.4421327.5ND1635000
PWZ-0854.86138.5ND0.5540
MMB-III-1413136.93331.1333
RY-06117136.7ND0.331
WZ-11319.213.213.4ND11.5300
YT-II-8332.7413.2224.1ND3.548ND
DM-II-30 (C20H13N3O2BrF3)17.613.428.51ND7.85000
LJD-III-15E1.931419ND70.81000
YT-III-272295.914.9810.77ND103.3ND
BCCt0.721518.9ND110.85000
XHE-II-006b3.7151218971441000
ABECARNIL12.415.37.5ND61000
MLT-II-347.0415.9522.3ND1581000
MSA-IV-352.11621ND9953000
JYI-04 (C21H23N3O3)28.316NDND0.511.57
PS-1-35 C23H22N5OBrND16.0324.41NDNDND
ZG69A6.816.39.2ND0.8554.6
ZG-69a (Ro15-1310)6.816.39.2ND0.8554.6
YT-III-42382.916.8344.04ND9.77ND
XHE-I-0657.2171850057500
XHE-II-073B (S-ENRICHED)111712332.1269
TJH-IV-512.3917.414.5ND31610000
SH-I-047171017.521222ND1519ND
XLi343 C20H19ClN2OSi6.37517.71NDND150.5ND
XHE-II-0028.318133.91.511
YT-III-38146118.2114.63ND3999
JYI-72 (C22H21N4SiF)48.518.5NDND11.55000
MSR-I-0326.218.74ND3.374.9
JC208 C15H10N2OS22.4218.89NDND5.039ND
diazepam142015ND11ND

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.