Assay Detail
Binding
CHEMBL868656
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Displacement of [3H]PGD2 from human CRTh2 expressed in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of potent CRTh2 (DP2) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.63 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378730 | — | — | 1 | 8.64 |
| CHEMBL209689 | — | — | 1 | 8.59 |
| CHEMBL214304 | — | — | 1 | 8.27 |
| CHEMBL214350 | — | — | 1 | 8.22 |
| CHEMBL213854 | — | — | 1 | 8.15 |
| CHEMBL212777 | — | — | 1 | 8.10 |
| CHEMBL211631 | — | — | 1 | 7.96 |
| CHEMBL211677 | — | — | 1 | 7.75 |
| CHEMBL213495 | — | — | 1 | 7.75 |
| CHEMBL378666 | — | — | 1 | 7.68 |
| CHEMBL213494 | — | — | 1 | 7.64 |
| CHEMBL379828 | — | — | 1 | 7.30 |
| CHEMBL384962 | — | — | 1 | 7.17 |
| CHEMBL378094 | — | — | 1 | 6.90 |
| CHEMBL213029 | — | — | 1 | 6.75 |
| CHEMBL379639 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378730 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL209689 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL214304 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL214350 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL213854 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL212777 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL211631 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL211677 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL213495 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL378666 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL213494 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL379828 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL384962 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL378094 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL213029 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL379639 | — | IC50 | = | 5200.0 | nM | 5.28 |