Assay Detail
Functional
CHEMBL1837510
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Inhibition of rabbit B1 receptor by cellular calcium flux assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.07 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834752 | — | — | 1 | 9.22 |
| CHEMBL1834619 | — | — | 1 | 8.96 |
| CHEMBL1834751 | — | — | 1 | 8.66 |
| CHEMBL1777958 | — | — | 1 | 8.39 |
| CHEMBL455642 | — | — | 1 | 7.95 |
| CHEMBL1834750 | — | — | 1 | 7.76 |
| CHEMBL1834616 | — | — | 1 | 7.67 |
| CHEMBL1834620 | — | — | 1 | 7.51 |
| CHEMBL1834749 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834752 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1834619 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1834751 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1777958 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL455642 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL1834750 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL1834616 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL1834620 | — | IC50 | = | 31.1 | nM | 7.51 |
| CHEMBL1834749 | — | IC50 | = | 342.3 | nM | 6.47 |