Table 1.
PDSP primary binding assay of DUQ0002 fractions. PDSP “hits” are highlighted in yellow and represent fractions showing >50% inhibition of binding. Data represented as mean % inhibition (N = 4 separate determinations). Negative inhibition represents stimulation of binding, meaning that the fraction increased binding of the standard compound from baseline. Abbreviations: mGluR5 – metabotropic glutamate receptor 5; DOR – delta opioid receptor, KOR – kappa opioid receptor; MOR- mu opioid receptor; SERT – serotonin transporter; NET – norepinephrine transporter; ND – not determined.
| DUQ0002 | 5-HT1A | 5-HT1B | 5-HT1D | 5-HT1E | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT3 | 5-HT5A | 5-HT6 | 5-HT7 | mGluR5 | DOR | KOR | MOR | SERT | NET |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A | −6.4 | −1.5 | −3.6 | −1.3 | −6.9 | −4.2 | −12.4 | 7.5 | −0.9 | −8.7 | −9.6 | ND | −16 | −8.6 | 7.7 | 91.7 | 9.2 |
| B | 3.7 | 9.8 | 12.1 | −7.2 | −9.2 | −7.9 | −12.7 | 15.1 | −4.8 | −10.9 | −13.4 | ND | −4.7 | −6.7 | −2.7 | 86.4 | 2.5 |
| C | 14.6 | 6.4 | 15.4 | −1.4 | −8.5 | 8.2 | −1.2 | 5.9 | 9.6 | 8.2 | 5.5 | 75.5 | 1.9 | −2.3 | 9.0 | 80.3 | 9.9 |
| D | 53.0 | 28.6 | 12.1 | 0.6 | 3.7 | 16.6 | 10.2 | 15.2 | 16.2 | 22.2 | 20.5 | 75.4 | 9.3 | 4.8 | 16.7 | 50.0 | 4.7 |
| E | 7.9 | 17.7 | 15.8 | −1.8 | −12.4 | 5.6 | −7.1 | 6.5 | 1.3 | 1.4 | −3.2 | 58.1 | 3.5 | 0.6 | 8.8 | 57.7 | 22.9 |
| F | −3.4 | 13.9 | 13.7 | 11.6 | −12.5 | 8.9 | −17.9 | 4.3 | −8.2 | −4.7 | −18.1 | 76.5 | 0.2 | 10.2 | 12.6 | 22.2 | 50.0 |
| G | 3.2 | 12.5 | 22.4 | 24.6 | −5.2 | 3.6 | −15.9 | 13.5 | −5.0 | −2.0 | −8.2 | 76.4 | 7.6 | 25.0 | 10.2 | 14.6 | 50.0 |
| H | 0.5 | −3.8 | 1.8 | 29.0 | 7.4 | 0.5 | −10.2 | 14.0 | 3.8 | 0.6 | −2.0 | 73.4 | 17.5 | 19.5 | 21.0 | −19.0 | 50.0 |
| I | 58.3 | 23.8 | 16.5 | 32.3 | 5.5 | 19.9 | 38.6 | 15.5 | 20.1 | 5.1 | 71.2 | 65.2 | 9.7 | 13.8 | 20.6 | 24.0 | 50.0 |