IRL790 IC50/Ki values for selected targets
| Assay | Radioligand (Type) | Source | IC50 (μM) | Ki (μM) | Reference Compound |
|---|---|---|---|---|---|
| D3 (h) | [3H]Me-spiperone (antagonist) | CHO | 0.41 | 0.09 | (+)butaclamol |
| D2S (h) | [3H]Me-spiperone (antagonist) | HEK-293 | 1.6 | 0.54 | (+)butaclamol |
| D2S (h) | [3H]7-OH-DPAT (agonist) | HEK-293 | 1.9 | 0.75 | 7-OH-DPAT |
| σ1 (h) | [3H](+)pentazocine (agonist) | Jurkat | 1.7 | 0.87 | Haloperidol |
| 5-HT1A (h) | [3H]8-OH-DPAT (agonist) | HEK-293 | 3.6 | 2.2 | 8-OH-DPAT |
| 5-HT2A (h) | [125I](±)DOI (agonist) | HEK-293 | 9.9 | 7.4 | (±) DOI |
| Norepinephrine transporter (h) | [3H]nisoxetine (inhibitor) | CHO | 11 | 8 | Protriptyline |
| 5-HT7 (h) | [3H]LSD (agonist) | CHO | 29 | 11 | Serotonin |
| α2C (h) | [3H]RX 821002 (antagonist) | CHO | 45 | 15 | Yohimbine |
| α1 (nonselective; rat) | [3H]prazosin (antagonist) | Rat cerebral cortex | >100 | — | Prazosin |
| α2A (h) | [3H]RX 821002 (antagonist) | CHO | >100 | — | Yohimbine |
| Dopamine transporter (h) | [3H]BTCP (antagonist) | >100 | — | BTCP | |
| H3 (h) | [3H]N-α-Me-histamine (agonist) | CHO | >100 | — | R(α)-Me-histamine |
| MAO-A (rat) | [3H]Ro 41-1049 (inhibitor) | Rat cerebral cortex | >100 | — | Clorgyline |
| MAO-B (rat) | [3H]Ro 19-6327 (inhibitor) | Rat cerebral cortex | >100 | — | (R)-deprenyl |
The abbreviation (h) denotes human recombinant protein. MAO, Monoamine oxidase; BTCP, N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine; 7-OH-DPAT, 7-hydroxy-2-(di-N-propylamino)tetralin; 8-OH-DPAT, 8-hydroxy-2-(di-n-propylamino)tetralin; DOI, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane; LSD, Lysergic acid diethyl amide