Assay Detail
Binding
CHEMBL1645647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human recombinant CRTH2 receptor by cell based radioligand equilibrium competition assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 41 | 8.07 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643780 | — | — | 1 | 9.00 |
| CHEMBL1643773 | — | — | 1 | 8.96 |
| CHEMBL1643774 | — | — | 1 | 8.96 |
| CHEMBL1643789 | — | — | 1 | 8.85 |
| CHEMBL179036 | — | — | 1 | 8.82 |
| CHEMBL1643783 | — | — | 1 | 8.80 |
| CHEMBL1643787 | — | — | 1 | 8.80 |
| CHEMBL1643775 | — | — | 1 | 8.77 |
| CHEMBL1643786 | — | — | 1 | 8.74 |
| CHEMBL1643778 | — | — | 1 | 8.62 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.60 |
| CHEMBL1643779 | — | — | 1 | 8.60 |
| CHEMBL1643782 | — | — | 1 | 8.43 |
| CHEMBL1643790 | — | — | 1 | 8.43 |
| CHEMBL1643784 | — | — | 1 | 8.40 |
| CHEMBL1643795 | — | — | 1 | 8.37 |
| CHEMBL1643798 | — | — | 1 | 8.36 |
| CHEMBL1643771 | — | — | 1 | 8.34 |
| CHEMBL1643788 | — | — | 1 | 8.31 |
| CHEMBL1643796 | — | — | 1 | 8.26 |
| CHEMBL298483 | — | — | 1 | 8.26 |
| CHEMBL1643768 | — | — | 1 | 8.22 |
| CHEMBL1643801 | — | — | 1 | 8.20 |
| CHEMBL1643792 | — | — | 1 | 8.12 |
| CHEMBL1643776 | — | — | 1 | 8.06 |
| CHEMBL1643794 | — | — | 1 | 8.06 |
| CHEMBL1643785 | — | — | 1 | 8.01 |
| CHEMBL1643770 | — | — | 1 | 7.96 |
| CHEMBL1643777 | — | — | 1 | 7.89 |
| CHEMBL1643791 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643780 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1643773 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1643774 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1643789 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL179036 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1643783 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1643787 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1643775 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1643786 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1643778 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1643779 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL561132 | MK-7246 | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1643782 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1643790 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1643784 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1643795 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1643798 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1643771 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL1643788 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL298483 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL1643796 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL1643768 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1643801 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL1643792 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL1643776 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL1643794 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL1643785 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL1643770 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1643777 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1643791 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1643800 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1643799 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1643793 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1643781 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1643797 | — | Ki | = | 40.8 | nM | 7.39 |
| CHEMBL1643804 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL1643802 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL361812 | RAMATROBAN | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL1643769 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL1643803 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL1643772 | CRTH2-negative-control | Ki | = | 1083.0 | nM | 5.96 |