High-affinity binding of pyrrolobenzoxazepines to homogenates of HL-60 cells
| Compound | Inhibition of [3H]PK11195 Binding to the PBR, Ki Value |
|---|---|
| nM | |
| PBOX-1 | 3.4 ± 0.2 |
| PBOX-2 | 1.2 ± 1.1 |
| PBOX-3 | 6.0 ± 1.9 |
| PBOX-4 | 1.9 ± 2.3 |
| PBOX-5 | 1.1 ± 0.9 |
| PBOX-6 | 6.7 ± 1.7 |
| PBOX-7 | 1.7 ± 0.7 |
Homogenates (50 μg of protein) of HL-60 cells were assayed for specific binding of [3H]PK11195 binding (2 nM) in the presence and absence of the indicated unlabeled displacing compound (0–1 μM). The amount of radioactivity bound in the presence of the displacer was expressed as a percentage of control binding and the values represent means ± S.E. of triplicate determinations from one representative experiment performed at least twice. TheKi values were obtained as described inExperimental Procedures.