Assay Detail
Functional
CHEMBL1645651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant CRTH2 receptor expressed in HEK293 cells assessed as inhibition of DK-PGD2-induced intracellular cAMP formation
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 37 | 7.86 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643783 | — | — | 1 | 8.60 |
| CHEMBL1643780 | — | — | 1 | 8.60 |
| CHEMBL1643773 | — | — | 1 | 8.59 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.52 |
| CHEMBL1643771 | — | — | 1 | 8.52 |
| CHEMBL1643774 | — | — | 1 | 8.52 |
| CHEMBL1643775 | — | — | 1 | 8.44 |
| CHEMBL1643779 | — | — | 1 | 8.42 |
| CHEMBL1643778 | — | — | 1 | 8.35 |
| CHEMBL1643787 | — | — | 1 | 8.31 |
| CHEMBL1643798 | — | — | 1 | 8.26 |
| CHEMBL1643789 | — | — | 1 | 8.24 |
| CHEMBL1643782 | — | — | 1 | 8.24 |
| CHEMBL1643788 | — | — | 1 | 8.17 |
| CHEMBL1643790 | — | — | 1 | 8.16 |
| CHEMBL1643786 | — | — | 1 | 8.09 |
| CHEMBL1643796 | — | — | 1 | 8.07 |
| CHEMBL1643776 | — | — | 1 | 8.05 |
| CHEMBL1643784 | — | — | 1 | 8.00 |
| CHEMBL1643795 | — | — | 1 | 7.92 |
| CHEMBL1643801 | — | — | 1 | 7.89 |
| CHEMBL1643794 | — | — | 1 | 7.89 |
| CHEMBL1643799 | — | — | 1 | 7.82 |
| CHEMBL1643791 | — | — | 1 | 7.66 |
| CHEMBL1643781 | — | — | 1 | 7.62 |
| CHEMBL1643800 | — | — | 1 | 7.60 |
| CHEMBL1643770 | — | — | 1 | 7.58 |
| CHEMBL1643792 | — | — | 1 | 7.57 |
| CHEMBL1643793 | — | — | 1 | 7.48 |
| CHEMBL1643785 | — | — | 1 | 7.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643783 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1643780 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1643773 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL561132 | MK-7246 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643771 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643774 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643775 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1643779 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1643778 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1643787 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1643798 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1643789 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1643782 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1643788 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL1643790 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1643786 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL1643796 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL1643776 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1643784 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL1643795 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1643801 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1643794 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1643799 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1643791 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1643781 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1643800 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1643770 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL1643792 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1643793 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1643785 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL1643777 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1643802 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1643797 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL1643803 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1643804 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL1643769 | — | IC50 | = | 864.0 | nM | 6.06 |
| CHEMBL1643772 | CRTH2-negative-control | IC50 | > | 10000.0 | nM | - |