Assay Detail
Functional
CHEMBL2168754
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Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.22 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164580 | — | — | 1 | 7.40 |
| CHEMBL2164576 | — | — | 1 | 7.38 |
| CHEMBL2164223 | — | — | 1 | 7.28 |
| CHEMBL2164582 | — | — | 1 | 7.28 |
| CHEMBL2164581 | — | — | 1 | 7.25 |
| CHEMBL2164577 | — | — | 1 | 7.20 |
| CHEMBL2164222 | — | — | 1 | 7.16 |
| CHEMBL2164579 | — | — | 1 | 7.11 |
| CHEMBL2164578 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164580 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2164576 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2164223 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2164582 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2164581 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2164577 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2164222 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2164579 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL2164578 | — | EC50 | = | 114.0 | nM | 6.94 |