Assay Detail
Functional
CHEMBL1920643
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Antagonist activity at human CRTH2 expressed in human CHO cells by cellular dielectric spectroscopy
4
Total Activities
4
Compounds Tested
2
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 | 7.33 | 7.55 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917592 | — | — | 1 | 7.55 |
| CHEMBL1917584 | — | — | 1 | 7.50 |
| CHEMBL1917389 | — | — | 1 | 6.94 |
| CHEMBL1917407 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917592 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1917584 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1917389 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL1917407 | — | Inhibition | = | 70.0 | % | - |