Off target protein and potency:
ORL-1 57.6 ± 8.0 nMPotency assay (off target):
Competitive radioligand binding assays using membranes prepared from clonal cell lines
Probe Selectivity in Vitro:
SB-612111 is highly selective versus μ-(174-fold), δ-(6391-fold), and κ (486-fold)-opioid receptors. Ki nM: μ- 57.6 ± 8.0, δ- 2109 ± 570, κ- 160.5 ± 22.4. SB-612111 was tested at a concentration of 10 μM by CEREP in a broad profile of radioligand binding assays specific for different classes of receptors, ion channels, and enzymes. The highest measured affinity interaction of SB-612111, to the β3-adrenergic receptor, was >260-fold weaker than its interaction with the ORL-1 receptor.
