Assay Detail
Binding
CHEMBL1102911
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Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK385-7 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK385-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.19 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088284 | — | — | 1 | 8.72 |
| CHEMBL603158 | — | — | 1 | 8.43 |
| CHEMBL1087029 | — | — | 1 | 8.36 |
| CHEMBL1087622 | — | — | 1 | 8.10 |
| CHEMBL1087031 | — | — | 1 | 7.82 |
| CHEMBL1080695 | — | — | 1 | 7.82 |
| CHEMBL1081033 | — | — | 1 | 7.75 |
| CHEMBL1087030 | — | — | 1 | 7.64 |
| CHEMBL1087501 | — | — | 1 | 7.37 |
| CHEMBL1088727 | — | — | 1 | 7.12 |
| CHEMBL1087500 | — | — | 1 | 7.08 |
| CHEMBL1086856 | — | — | 1 | 7.08 |
| CHEMBL1076716 | — | — | 1 | 6.72 |
| CHEMBL1080393 | — | — | 1 | 5.90 |
| CHEMBL1088285 | — | — | 1 | 5.68 |
| CHEMBL1080560 | — | — | 1 | 5.55 |
| CHEMBL1086857 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088284 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL603158 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1087029 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1087622 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1087031 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1080695 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1081033 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1087030 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1087501 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1088727 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1087500 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1086856 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1076716 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1080393 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL1088285 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL1080560 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL1086857 | — | IC50 | = | 9140.0 | nM | 5.04 |