Assay Detail
Binding
CHEMBL1051055
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Displacement of [3H]PGD2 from human CRTh2 receptor expressed in CHO cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.82 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL563949 | — | — | 1 | 7.51 |
| CHEMBL559316 | — | — | 1 | 7.46 |
| CHEMBL559044 | — | — | 1 | 7.44 |
| CHEMBL557662 | — | — | 1 | 7.37 |
| CHEMBL557457 | — | — | 1 | 7.32 |
| CHEMBL560279 | — | — | 1 | 7.28 |
| CHEMBL562339 | — | — | 1 | 7.25 |
| CHEMBL398126 | — | — | 1 | 7.23 |
| CHEMBL361812 | RAMATROBAN | 4.0 | 1 | 7.14 |
| CHEMBL561539 | — | — | 1 | 6.99 |
| CHEMBL551274 | — | — | 1 | 6.80 |
| CHEMBL549587 | — | — | 1 | 6.55 |
| CHEMBL564002 | — | — | 1 | 6.42 |
| CHEMBL561942 | — | — | 1 | 6.21 |
| CHEMBL549793 | — | — | 1 | 5.93 |
| CHEMBL565106 | — | — | 1 | 5.58 |
| CHEMBL562593 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL563949 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL559316 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL559044 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL557662 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL557457 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL560279 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL562339 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL398126 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL361812 | RAMATROBAN | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL561539 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL551274 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL549587 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL564002 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL561942 | — | Ki | = | 619.0 | nM | 6.21 |
| CHEMBL549793 | — | Ki | = | 1171.0 | nM | 5.93 |
| CHEMBL565106 | — | Ki | = | 2619.0 | nM | 5.58 |
| CHEMBL562593 | — | Ki | = | 3220.0 | nM | 5.49 |