Assay Detail
Functional
CHEMBL1920641
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Antagonist activity human CRTH2 expressed in chinese hamster CHO cells assessed as inhibition of PGD2-induced [35S]GTPgamma binding by liquid scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.74 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917584 | — | — | 1 | 8.15 |
| CHEMBL1917592 | — | — | 1 | 8.10 |
| CHEMBL1917389 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917584 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1917592 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1917389 | — | IC50 | = | 104.0 | nM | 6.98 |