Table 1.
Radioligand Displacement by NYX-2925 (10 μM)
| Site | NYX-2925
% Inhibition |
|---|---|
| A1 (antagonist) | -4.2 |
| A2A (agonist) | -6.1 |
| A3 (agonist) | -4.9 |
| α1 non-selective (antagonist) | -10 |
| α2 non-selective (antagonist) | -11.6 |
| β1 (agonist) | 4.6 |
| β2 (agonist) | -7.6 |
| AT1 (antagonist) | -0.8 |
| AT2 (agonist) | 1.8 |
| BZD central (agonist) | -9.1 |
| BZD peripheral (antagonist) | -6.6 |
| BB non-selective (agonist) | -9 |
| B2 (agonist) | -3.1 |
| CGRP (agonist) | 3.6 |
| CB1 (agonist) | 5.7 |
| CCK1 CCKA (agonist) | 3.8 |
| CCK2 CCKB (agonist) | -13 |
| D1 (antagonist) | -19.9 |
| D2S (antagonist) | 6.8 |
| D3 (antagonist) | -5.2 |
| D4.4 (antagonist) | -5 |
| D5 (antagonist) | 4.1 |
| ETA (agonist) | 5.7 |
| ETB (agonist) | 1.3 |
| GABA non-selective (agonist) | -18.8 |
| GAL1 (agonist) | 3 |
| GAL2 (agonist) | 3.7 |
| PDGF (agonist) | -2.6 |
| CXCR2 IL-8B (agonist) | -4.5 |
| CCR1 (agonist) | 0 |
| TNF-α (agonist) | -21.7 |
| H1 (antagonist) | 2.4 |
| H2 (antagonist) | 0.5 |
| MC4 (agonist) | 3.4 |
| MT1 ML1A (agonist) | 1.4 |
| M1 (antagonist) | -23.4 |
| M2 (antagonist) | -6.1 |
| M3 (antagonist) | -10.1 |
| M4 (antagonist) | -11.3 |
| M5 (antagonist) | 5.6 |
| NK1 (agonist) | -22.5 |
| NK2 (agonist) | 2.4 |
| NK3 (antagonist) | -7.7 |
| Y1 (agonist) | -3.4 |
| Y2 (agonist) | -9.9 |
| NTS1 / NT1 (agonist) | -11.4 |
| δ2 (DOP) (agonist) | -4.2 |
| κ (KOP) (agonist) | 0.1 |
| μ (MOP) (agonist) | -4.5 |
| NOP / ORL1 (agonist) | 5.9 |
| PAC1 / PACAP (agonist) | -4.4 |
| PPARγ (agonist) | -10.7 |
| PCP (antagonist) | -5.7 |
| EP2 (agonist) | 4.7 |
| EP4 (agonist) | 7.5 |
| IP PGI2 (agonist) | -5.1 |
| P2X (agonist) | 16.1 |
| P2Y (agonist) | 5.1 |
| 5-HT1A (agonist) | 2.5 |
| 5-HT1B (antagonist) | -6.7 |
| 5-HT2A (antagonist) | -5.8 |
| 5-HT2B (agonist) | 2.1 |
| 5-HT2C (antagonist) | -5.9 |
| 5-HT3 (antagonist) | 2.7 |
| 5-HT5a (agonist) | -7.5 |
| 5-HT6 (agonist) | -8.6 |
| 5-HT7 (agonist) | -5.1 |
| Sigma (non-selective) (agonist) | -15.8 |
| SSST (non-selective) (agonist) | -13.8 |
| GR (agonist) | -6.2 |
| VPAC1 (VIP1) (agonist) | 7.4 |
| V1 a (agonist) | 15.3 |
| Verapamil site (antagonist) | 3.4 |
| hERG [3H] Dofetilide | -3 |
| KV channel (antagonist) | -7.4 |
| SKCa channel (antagonist) | 5 |
| Na+ channel (site 2) (antagonist) | 7.3 |
| Cl- channel GABA-gated (antagonist) | 5.2 |
| Norepinephrine transporter (antagonist) | -6.2 |
| Dopamine transporter (antagonist) | -6.4 |
| 5-HT transporter (antagonist) | -13.9 |
Results that show an inhibition or stimulation >50%
are considered to represent significant effects of the test compound.