Potency data for probe CRTH2 antagonist and control CRTH2 negative control
In vitro potency
| Target name | Target information | Species | Assay description | CRTH2 antagonist | CRTH2 negative control | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PTGDR2 | Homo sapiens | Prostanoid receptor binding assay (PTGDR2) | Ki = 2.5 nM | Ki = 1083 nM | PMID: 10634944 | |
| SLC6A3 | Homo sapiens | Prostanoid receptor binding assay (SLC6A3) | Ki = 373 nM | Ki > 3235 nM | PMID: 10634944 | |
| TBXA2R | Homo sapiens | Prostanoid receptor binding assay (TBXA2R) | Ki = 3804 nM | Ki > 6489 nM | PMID: 10634944 |
In cell potency
| Target name | Target information | Species | Assay description | CRTH2 antagonist | CRTH2 negative control | Publication of assay conditions |
|---|---|---|---|---|---|---|
| PTGDR2 | HEK-hCRTH2 cells | Homo sapiens | cAMP Functional Assay | IC50 = 3 nM | IC50 > 10 µM | PMID: 12466225 |
| PTGDR2 | Homo sapiens | Functional Assay: Eosinophil Shape Change (whole blood) | IC50 = 2.2 nM | |||
| PTGDR2 | Homo sapiens | Functional Assay: Eosinophil CD11b (whole blood) | IC50 = 2.3 nM | |||
| SLC6A3 | Homo sapiens | Functional Assay: Platelet-rich plasma SLC6A3/cAMP | IC50 = 8692 nM |