Assay Detail
Binding
CHEMBL1944119
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Displacement of [3H]PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Chemoattractant receptor-homologous molecule expressed on Th2 cells (CHEMBL1075058) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Discovery of novel and potent CRTH2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.79 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1941129 | — | — | 1 | 7.77 |
| CHEMBL1941128 | — | — | 1 | 7.75 |
| CHEMBL1941127 | — | — | 1 | 7.28 |
| CHEMBL1941126 | — | — | 1 | 7.00 |
| CHEMBL1941123 | — | — | 1 | 6.89 |
| CHEMBL1941117 | — | — | 1 | 6.83 |
| CHEMBL1941121 | — | — | 1 | 6.68 |
| CHEMBL1941116 | — | — | 1 | 6.59 |
| CHEMBL1941118 | — | — | 1 | 6.45 |
| CHEMBL1941120 | — | — | 1 | 6.11 |
| CHEMBL1941122 | — | — | 1 | 6.10 |
| CHEMBL1941124 | — | — | 1 | 6.00 |
| CHEMBL1941119 | — | — | 1 | - |
| CHEMBL1941125 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1941129 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1941128 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1941127 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1941126 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1941123 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL1941117 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL1941121 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL1941116 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL1941118 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL1941120 | — | IC50 | = | 772.0 | nM | 6.11 |
| CHEMBL1941122 | — | IC50 | = | 797.0 | nM | 6.10 |
| CHEMBL1941124 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1941119 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1941125 | — | IC50 | > | 1000.0 | nM | - |