Kinetic and equilibrium binding parameters of unlabeled QAW039 and other CRTh2 ligands interacting with the human CRTh2 receptor
Data are mean ± S.E.M. from at least three separate experiments.
| CRTh2 Ligand | kon | koff | t1/2 | Kinetic pKd | Equilibrium pKi |
|---|---|---|---|---|---|
| M-1min−1 | min−1 | min | |||
| QAW039 | 6.27 ± 0.93 × 107 | 0.061 ± 0.006 | 12.04 | 8.99 ± 0.06 | 8.98 ± 0.03 |
| QAV680 | 4.80 ± 2.14 × 107 | 0.66 ± 0.18 | 1.29 | 7.82 ± 0.04 | 7.54 ± 0.09 |
| AZD-1981 | 3.01 ± 0.76 × 108 | 0.77 ± 0.23 | 1.26 | 7.58 ± 0.02 | 8.49 ± 0.03 |
| OC-459 | 9.50 ± 5.14 × 108 | 1.83 ± 0.32 | 0.41 | 8.61 ± 0.17 | 8.35 ± 0.13 |
| BI-671800 | 2.47 ± 0.36 × 108 | 1.22 ± 0.11 | 0.58 | 8.30 ± 0.01 | 8.14 ± 0.20 |
| Ramatroban | 1.89 ± 0.66 × 107 | 0.80 ± 0.22 | 1.10 | 7.33 ± 0.05 | 7.45 ± 0.02 |
| Setipiprant | 1.87 ± 0.45 × 108 | 0.95 ± 0.15 | 0.76 | 8.28 ± 0.04 | 8.35 ± 0.06 |
| PGD2 | nd | nd | nd | nd | 6.41 ± 0.08 |
| Indomethacin | nd | nd | nd | nd | 5.74 ± 0.12 |
nd, Not determined.