Assay Detail
Functional
CHEMBL1645652
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Antagonist activity at CRTH2 receptor in human whole blood assessed as inhibition of DK-PGD2-induced eosinophils shape change
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.10 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643780 | — | — | 1 | 8.96 |
| CHEMBL1643773 | — | — | 1 | 8.85 |
| CHEMBL1643785 | — | — | 1 | 8.80 |
| CHEMBL1643783 | — | — | 1 | 8.74 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.66 |
| CHEMBL1643789 | — | — | 1 | 8.39 |
| CHEMBL1643777 | — | — | 1 | 8.30 |
| CHEMBL1643775 | — | — | 1 | 7.97 |
| CHEMBL1643771 | — | — | 1 | 7.94 |
| CHEMBL1643774 | — | — | 1 | 7.94 |
| CHEMBL1643784 | — | — | 1 | 7.85 |
| CHEMBL1643778 | — | — | 1 | 7.52 |
| CHEMBL1643787 | — | — | 1 | 6.97 |
| CHEMBL1643769 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643780 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1643773 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1643785 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1643783 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL561132 | MK-7246 | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1643789 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1643777 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1643775 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL1643771 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL1643774 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL1643784 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL1643778 | — | IC50 | = | 30.5 | nM | 7.52 |
| CHEMBL1643787 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL1643769 | — | IC50 | = | 325.0 | nM | 6.49 |