Table 1.
Ligand | Ki for TMEM97 in Sf9 cells, nM | σ2 Ki, nM |
DTG | 19.6 ± 3.0 | 21.2* |
Haloperidol | 54.1 ± 6.7 | 48.7* |
PB-28 | 2.0 ± 0.3 | 1.8† |
(+)-pentazocine | 2,467 ± 436 | 1,402* – 3,890† |
(+)-SKF 10,047 | >10,000 | No inhibition* |
SAS-1121 | 25.2 ± 3.8 | 23.8‡ |
Elacridar | 6.5 ± 1.1 | 4.7 ± 0.7 |
Ro 48-8071 | 971 ± 228 | 817 ± 226 |
The inhibition constant (Ki) for various ligands binding to recombinant TMEM97 and to the σ2 receptor natively expressed in cell membranes. Affinities were measured as described in Methods and are reported from literature where indicated.
Data from Hellewell and Bowen, 1990 (3).
Data from Colabufo et al., 2004 (49).
Data from Sahn et al., 2017 (20).