Assay Detail
Functional
CHEMBL3387261
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Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.70 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354618 | — | — | 1 | 10.82 |
| CHEMBL3354616 | — | — | 1 | 10.28 |
| CHEMBL3354614 | — | — | 1 | 8.41 |
| CHEMBL3354615 | — | — | 1 | 8.19 |
| CHEMBL3335473 | — | — | 1 | 7.97 |
| CHEMBL3354613 | — | — | 1 | 7.95 |
| CHEMBL2107786 | TERUTROBAN | 3.0 | 1 | 7.79 |
| CHEMBL3354619 | — | — | 1 | 7.54 |
| CHEMBL3335482 | — | — | 1 | 7.23 |
| CHEMBL65121 | — | — | 1 | 6.28 |
| CHEMBL3335481 | — | — | 1 | 6.05 |
| CHEMBL3335483 | — | — | 1 | 6.05 |
| CHEMBL3354617 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354618 | — | IC50 | = | 0.015 | nM | 10.82 |
| CHEMBL3354616 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL3354614 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3354615 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3335473 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL3354613 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL2107786 | TERUTROBAN | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL3354619 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL3335482 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL65121 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL3335481 | — | IC50 | = | 891.0 | nM | 6.05 |
| CHEMBL3335483 | — | IC50 | = | 892.0 | nM | 6.05 |
| CHEMBL3354617 | — | IC50 | = | 2760.0 | nM | 5.56 |