In vitro pharmacology assaysQAW039 (nM)QAV680 (nM)
HCRTh2 radioligand binding (Ki)4.7±2.029±8.0
HCRTh2 cAMP functional -HSA (IC50)36.9±1097.1±12
HCRTh2 cAMP functional +HSA (IC50)31.5±4.813±22
Human isolated ESC (PGD2) (IC50)0.4±0.043.6±0.19
Human isolated ESC (DK-PGD2) (IC50)0.4±0.093.3±0.43
Human whole blood ESC (PGD2) (IC50)0.77±0.3050.3±14.4
IL-5 production (IC50)2.9±1.359±28
IL-13 production (IC50)1.4±0.525±4.9
  • HCRTh2- Human CRTh2