Assay Detail
Functional
CHEMBL1680282
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Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
8
Total Activities
8
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-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.20 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1671874 | — | — | 1 | 7.85 |
| CHEMBL1672354 | — | — | 1 | 7.85 |
| CHEMBL1672353 | — | — | 1 | 7.80 |
| CHEMBL1091720 | — | — | 1 | 7.33 |
| CHEMBL1093184 | — | — | 1 | 7.18 |
| CHEMBL1672352 | — | — | 1 | 7.17 |
| CHEMBL1672351 | — | — | 1 | 6.66 |
| CHEMBL1079517 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1671874 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1672354 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1672353 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1091720 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1093184 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1672352 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1672351 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1079517 | — | EC50 | = | 1900.0 | nM | 5.72 |