Assay Detail
Binding
CHEMBL1645649
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Binding affinity to thromboxane receptor
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 | 6.07 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361812 | RAMATROBAN | 4.0 | 1 | 9.24 |
| CHEMBL1643785 | — | — | 1 | 7.96 |
| CHEMBL298483 | — | — | 1 | 7.28 |
| CHEMBL1643784 | — | — | 1 | 6.37 |
| CHEMBL1643779 | — | — | 1 | 6.14 |
| CHEMBL1643773 | — | — | 1 | 6.14 |
| CHEMBL1643770 | — | — | 1 | 6.05 |
| CHEMBL1643787 | — | — | 1 | 6.04 |
| CHEMBL1643780 | — | — | 1 | 6.02 |
| CHEMBL1643796 | — | — | 1 | 5.98 |
| CHEMBL1643788 | — | — | 1 | 5.91 |
| CHEMBL1643781 | — | — | 1 | 5.88 |
| CHEMBL1643790 | — | — | 1 | 5.87 |
| CHEMBL1643768 | — | — | 1 | 5.86 |
| CHEMBL1643775 | — | — | 1 | 5.82 |
| CHEMBL1643789 | — | — | 1 | 5.80 |
| CHEMBL1643782 | — | — | 1 | 5.74 |
| CHEMBL1643771 | — | — | 1 | 5.73 |
| CHEMBL1643786 | — | — | 1 | 5.67 |
| CHEMBL1643797 | — | — | 1 | 5.67 |
| CHEMBL1643783 | — | — | 1 | 5.67 |
| CHEMBL1643801 | — | — | 1 | 5.55 |
| CHEMBL1643778 | — | — | 1 | 5.54 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 5.42 |
| CHEMBL1643774 | — | — | 1 | 5.40 |
| CHEMBL179036 | — | — | 1 | 5.16 |
| CHEMBL1643804 | — | — | 1 | - |
| CHEMBL1643803 | — | — | 1 | - |
| CHEMBL1643802 | — | — | 1 | - |
| CHEMBL1643769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361812 | RAMATROBAN | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1643785 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL298483 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL1643784 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL1643779 | — | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL1643773 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL1643770 | — | Ki | = | 888.0 | nM | 6.05 |
| CHEMBL1643787 | — | Ki | = | 904.0 | nM | 6.04 |
| CHEMBL1643780 | — | Ki | = | 962.0 | nM | 6.02 |
| CHEMBL1643796 | — | Ki | = | 1039.0 | nM | 5.98 |
| CHEMBL1643788 | — | Ki | = | 1222.0 | nM | 5.91 |
| CHEMBL1643781 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL1643790 | — | Ki | = | 1357.0 | nM | 5.87 |
| CHEMBL1643768 | — | Ki | = | 1394.0 | nM | 5.86 |
| CHEMBL1643775 | — | Ki | = | 1518.0 | nM | 5.82 |
| CHEMBL1643789 | — | Ki | = | 1569.0 | nM | 5.80 |
| CHEMBL1643782 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL1643771 | — | Ki | = | 1872.0 | nM | 5.73 |
| CHEMBL1643783 | — | Ki | = | 2152.0 | nM | 5.67 |
| CHEMBL1643786 | — | Ki | = | 2142.0 | nM | 5.67 |
| CHEMBL1643797 | — | Ki | = | 2118.0 | nM | 5.67 |
| CHEMBL1643801 | — | Ki | = | 2840.0 | nM | 5.55 |
| CHEMBL1643778 | — | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL561132 | MK-7246 | Ki | = | 3804.0 | nM | 5.42 |
| CHEMBL1643774 | — | Ki | = | 3949.0 | nM | 5.40 |
| CHEMBL179036 | — | Ki | = | 6852.0 | nM | 5.16 |
| CHEMBL1643777 | — | Ki | > | 7247.0 | nM | - |
| CHEMBL1643776 | — | Ki | > | 7139.0 | nM | - |
| CHEMBL1643791 | — | Ki | > | 21160.0 | nM | - |
| CHEMBL1643792 | — | Ki | > | 5591.0 | nM | - |
| CHEMBL1643793 | — | Ki | > | 7054.0 | nM | - |
| CHEMBL1643794 | — | Ki | > | 5591.0 | nM | - |
| CHEMBL1643795 | — | Ki | > | 7054.0 | nM | - |
| CHEMBL1643772 | CRTH2-negative-control | Ki | > | 6489.0 | nM | - |
| CHEMBL1643798 | — | Ki | > | 7096.0 | nM | - |
| CHEMBL1643799 | — | Ki | > | 5591.0 | nM | - |
| CHEMBL1643800 | — | Ki | > | 5745.0 | nM | - |
| CHEMBL1643769 | — | Ki | > | 21660.0 | nM | - |
| CHEMBL1643802 | — | Ki | > | 7181.0 | nM | - |
| CHEMBL1643803 | — | Ki | > | 7054.0 | nM | - |
| CHEMBL1643804 | — | Ki | > | 7181.0 | nM | - |