Assay Detail
Functional
CHEMBL1051797
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Antagonist activity against CRTh2 receptor in human whole blood assessed as eosinophil shape change
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 |
|---|---|---|---|
| IC50 | 9 | 7.02 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL563949 | — | — | 1 | 7.77 |
| CHEMBL559044 | — | — | 1 | 7.40 |
| CHEMBL559316 | — | — | 1 | 7.25 |
| CHEMBL562339 | — | — | 1 | 6.81 |
| CHEMBL361812 | RAMATROBAN | 4.0 | 1 | 6.71 |
| CHEMBL560279 | — | — | 1 | 6.20 |
| CHEMBL551274 | — | — | 1 | - |
| CHEMBL557662 | — | — | 1 | - |
| CHEMBL398126 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL563949 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL559044 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL559316 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL562339 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL361812 | RAMATROBAN | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL560279 | — | IC50 | = | 629.0 | nM | 6.20 |
| CHEMBL551274 | — | IC50 | - | — | - | |
| CHEMBL557662 | — | IC50 | - | — | - | |
| CHEMBL398126 | — | IC50 | > | 10000.0 | nM | - |