Assay Detail
Functional
CHEMBL1116183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.72 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089721 | — | — | 1 | 7.60 |
| CHEMBL1092381 | — | — | 1 | 7.43 |
| CHEMBL1082471 | — | — | 1 | 7.36 |
| CHEMBL1091720 | — | — | 1 | 7.33 |
| CHEMBL1092730 | — | — | 1 | 7.20 |
| CHEMBL1093459 | — | — | 1 | 7.20 |
| CHEMBL1093184 | — | — | 1 | 7.18 |
| CHEMBL1091985 | — | — | 1 | 6.98 |
| CHEMBL1091599 | — | — | 1 | 6.88 |
| CHEMBL1089521 | — | — | 1 | 6.87 |
| CHEMBL1093170 | — | — | 1 | 6.77 |
| CHEMBL1091918 | — | — | 1 | 6.77 |
| CHEMBL1093183 | — | — | 1 | 6.71 |
| CHEMBL1091984 | — | — | 1 | 6.52 |
| CHEMBL1091917 | — | — | 1 | 6.38 |
| CHEMBL1091598 | — | — | 1 | 6.37 |
| CHEMBL1089512 | — | — | 1 | 6.37 |
| CHEMBL1089511 | — | — | 1 | 6.27 |
| CHEMBL1089522 | — | — | 1 | 6.24 |
| CHEMBL1089523 | — | — | 1 | 6.19 |
| CHEMBL1091553 | — | — | 1 | 5.90 |
| CHEMBL1091554 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089721 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1092381 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1082471 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1091720 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1092730 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1093459 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1093184 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1091985 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1091599 | — | EC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1089521 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1093170 | — | EC50 | = | 169.0 | nM | 6.77 |
| CHEMBL1091918 | — | EC50 | = | 171.0 | nM | 6.77 |
| CHEMBL1093183 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL1091984 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL1091917 | — | EC50 | = | 422.0 | nM | 6.38 |
| CHEMBL1091598 | — | EC50 | = | 425.0 | nM | 6.37 |
| CHEMBL1089512 | — | EC50 | = | 431.0 | nM | 6.37 |
| CHEMBL1089511 | — | EC50 | = | 538.0 | nM | 6.27 |
| CHEMBL1089522 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1089523 | — | EC50 | = | 641.0 | nM | 6.19 |
| CHEMBL1091553 | — | EC50 | = | 1263.0 | nM | 5.90 |
| CHEMBL1091554 | — | EC50 | = | 5234.0 | nM | 5.28 |