TABLE 1

IRL752 IC50/Ki values for selected human target proteins

For assay details, see https://www.eurofinsdiscoveryservices.com/cms/cms-content/services/in-vitro-assays/.

AssayRadioligand (Type)IC50 (μM)Ki (μM)
5-HT7 (h)[3H]-LSD (agonist)2.70.98
σ1 (h)[3H]-(+)pentazocine (agonist)2.41.2
Serotonin transporter, SERT (h)[3H]-imipramine (inhibitor)5.42.5
α2C (h)[3H]-RX 821002 (antagonist)123.8
α2A (h)[3H]-RX 821002 (antagonist)156.5
5-HT2C (h)[125I]-(±)DOI (agonist)7.36.6
5-HT2A (h)[125I]-(±)DOI (agonist)118.1
Noradrenaline transporter, NAT (h)[3H]-nisoxetine (inhibitor)118.1
  • h, human; LSD, lysergic acid diethylamide; DOI, 2,5-Dimethoxy-4-iodoamphetamine.