Agonistic and antagonistic activities of E6130 (10 μM) toward chemokine receptors
| Receptor | Agonist Mode % Activationb | Antagonist Mode % Inhibition |
|---|---|---|
| [35S]GTPγS bindinga | ||
| CCR1 | 1.6 | 15.1 |
| CCR2 | 3.1 | 24.9 |
| CCR3 | −8.1 | 54.8 |
| CCR4 | −6.1 | 44.0 |
| CCR6 | −5.2 | 18.7 |
| CCR7 | 0.9 | −15.2 |
| CCR8 | 8.9 | 9.7 |
| CCR10 | −5.1 | 9.1 |
| CX3CR1 | 95.2 | −18.6 |
| CXCR1 | −2.2 | 23.3 |
| CXCR2 | −3.4 | 9.1 |
| CXCR3 | 2.4 | 22.7 |
| CXCR4 | 0.0 | 13.2 |
| CXCR6 | −1.3 | 10.9 |
| XCR1 | −4.3 | 23.8 |
| β-arrestinc | ||
| CCR2 | −3 | −13 |
| CCR3 | −2 | 5 |
| CCR4 | −2 | −11 |
| CCR5 | −2 | 0 |
| CCR6 | −2 | 2 |
| CCR7 | −5 | 10 |
| CCR8 | −1 | 15 |
| CCR9 | −3 | 6 |
| CCR10 | −1 | −15 |
| CX3CR1 | 179 | 0 |
| CXCR1 | −1 | −10 |
| CXCR2 | −1 | 6 |
| CXCR3 | −1 | −2 |
| CXCR4 | 3 | 10 |
| CXCR5 | −2 | 4 |
| CXCR6 | 1 | −10 |
| ACKR3/CMKOR1 | 157 | 0 |
ACKR3/CMKOR1, atypical chemokine receptor 3/chemokine orphan receptor 1.
↵a GTPγS binding assay was performed for chemokine receptors.
↵b Agonist activity of E6130 is expressed as a percentage of the activity of the reference agonists at their EC100 concentrations.
↵c PathHunter β-arrestin assay was performed for chemokine/chemokine-like receptors.