Assay Detail
Binding
CHEMBL2182589
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Inhibition of CRTH2
14
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.91 | 9.30 |
| IC50 | 6 | 8.53 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181748 | — | — | 1 | 10.70 |
| CHEMBL2181751 | — | — | 1 | 9.30 |
| CHEMBL1643768 | — | — | 2 | 9.22 |
| CHEMBL1080199 | — | — | 1 | 8.52 |
| CHEMBL2181750 | — | — | 1 | 8.32 |
| CHEMBL2181753 | AM-211 | 1.0 | 1 | 8.31 |
| CHEMBL2181754 | — | — | 1 | 7.87 |
| CHEMBL2181813 | — | — | 1 | 7.75 |
| CHEMBL2181812 | — | — | 1 | 7.47 |
| CHEMBL1917462 | — | — | 1 | 7.24 |
| CHEMBL2181743 | — | — | 1 | 6.97 |
| CHEMBL2181745 | — | — | 1 | 6.42 |
| CHEMBL2181752 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181748 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL2181751 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1643768 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1080199 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1643768 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2181750 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL2181753 | AM-211 | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2181754 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2181813 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2181812 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1917462 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2181743 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL2181745 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL2181752 | — | Ki | < | 1000.0 | nM | - |