In vitro pharmacology assays | QAW039 (nM) | QAV680 (nM) |
HCRTh2 radioligand binding (Ki) | 4.7±2.0 | 29±8.0 |
HCRTh2 cAMP functional -HSA (IC50) | 36.9±10 | 97.1±12 |
HCRTh2 cAMP functional +HSA (IC50) | 31.5±4.8 | 13±22 |
Human isolated ESC (PGD2) (IC50) | 0.4±0.04 | 3.6±0.19 |
Human isolated ESC (DK-PGD2) (IC50) | 0.4±0.09 | 3.3±0.43 |
Human whole blood ESC (PGD2) (IC50) | 0.77±0.30 | 50.3±14.4 |
IL-5 production (IC50) | 2.9±1.3 | 59±28 |
IL-13 production (IC50) | 1.4±0.5 | 25±4.9 |
HCRTh2- Human CRTh2