Table 3. CPL302-253 selectivity in SafetyScan44 panel.
Genetically modified reporter cell lines were treated with CPL302-253 at 10μM. G Protein-Coupled Receptors (GPCR), transporters, ion channels, nuclear receptors, kinases and non-kinase enzymes activity was measured in corresponding cell model. The CPL302-253 influence on measured parameter is indicated as % of response in control conditions.
| Gene symbol | Assay mode | CPL302-253 10 μM % Response |
|---|---|---|
| GPCRs | ||
| ADORA2A | Agonist | -0.8 |
| ADORA2A | Antagonist | 11.7 |
| ADRA1A | Agonist | -22.5 |
| ADRA1A | Antagonist | -2.8 |
| ADRA2A | Agonist | 0.4 |
| ADRA2A | Antagonist | -0.7 |
| ADRB1 | Agonist | 0.5 |
| ADRB1 | Antagonist | 26.6 |
| ADRB2 | Agonist | 0.5 |
| ADRB2 | Antagonist | 17.7 |
| AVPR1A | Agonist | -3.2 |
| AVPR1A | Antagonist | -5.2 |
| CCKAR | Agonist | -2.8 |
| CCKAR | Antagonist | -2.4 |
| CHRM1 | Agonist | 1.2 |
| CHRM1 | Antagonist | 48.1 |
| CHRM2 | Agonist | 8.2 |
| CHRM2 | Antagonist | 35.2 |
| CHRM3 | Agonist | 1.2 |
| CHRM3 | Antagonist | 12.6 |
| CNR1 | Agonist | -9.2 |
| CNR1 | Antagonist | -1.3 |
| CNR2 | Agonist | 16.4 |
| CNR2 | Antagonist | 1.1 |
| DRD1 | Agonist | 1.1 |
| DRD1 | Antagonist | 9.3 |
| DRD2S | Agonist | -4.5 |
| DRD2S | Antagonist | -1.1 |
| EDNRA | Agonist | -3.3 |
| EDNRA | Antagonist | -4.8 |
| HRH1 | Agonist | -0.2 |
| HRH1 | Antagonist | 7.2 |
| HRH2 | Agonist | 0.6 |
| HRH2 | Antagonist | 4.2 |
| HTR1A | Agonist | 5.6 |
| HTR1A | Antagonist | -4.8 |
| HTR1B | Agonist | 8.0 |
| HTR1B | Antagonist | 0.1 |
| HTR2A | Agonist | -1.5 |
| HTR2A | Antagonist | 11.5 |
| HTR2B | Agonist | 1.5 |
| HTR2B | Antagonist | 12.6 |
| OPRD1 | Agonist | -6.4 |
| OPRD1 | Antagonist | 0.4 |
| OPRK1 | Agonist | -11.0 |
| OPRK1 | Antagonist | 0.3 |
| OPRM1 | Agonist | -9.0 |
| OPRM1 | Antagonist | 0.2 |
| Nuclear Hormone Receptors | ||
| AR | Agonist | -0.7 |
| AR | Antagonist | 8.5 |
| GR | Agonist | 0.0 |
| GR | Antagonist | -5.6 |
| Transporters | ||
| DAT | Blocker | 56.1 |
| NET | Blocker | 8.5 |
| SERT | Blocker | 21.5 |
| Ion Channels | ||
| CAV1.2 | Blocker | -1.1 |
| GABAA | Opener | -2.3 |
| GABAA | Blocker | 1.4 |
| hERG | Blocker | -2.7 |
| HTR3A | Opener | -0.8 |
| HTR3A | Blocker | 19.5 |
| NAV1.5 | Blocker | 9.7 |
| Non-Kinase Enzymes | ||
| AChE | Inhibitor | 27.8 |
| COX1 | Inhibitor | 4.7 |
| COX2 | Inhibitor | 11.9 |
| MAOA | Inhibitor | 8.5 |
| PDE3A | Inhibitor | -8.1 |
| PDE4D2 | Inhibitor | 2.0 |
| Kinases | ||
| INSR | Inhibitor | -6.5 |
| LCK | Inhibitor | 16.3 |
| ROCK1 | Inhibitor | 10.3 |
| VEGFR2 | Inhibitor | 30.7 |