Table 8: Ligands with potent affinity for 4; 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
XHE-III-7477105380.422.25.8
TG-4-292.83.92.72.10.183.9
SVO-8-301.15.35.32.80.615
XHE-II-0028.318133.91.511
XHE-III-06a12151.837
RY-080 C17H15N3O328.421.425.85.30.4928.8
TG-4-391.634245.61.423
SVO-8-1482586.90.914
RY-023 C22H27N3O3Si197142.62557.82.6158.6
MMB-II-9020245.790.2536
XHE-III-142.6101327
XHE-II-0240.090.180.32140.2411
XHE-II-073A (R ENRICHED)5.91110151.18140
SVO-8-6774126152.3191
CM-B31i (ss)9018478184.9121
SVO-8-20114028198.6138

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.