Assay Detail
Functional
CHEMBL1110002
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Agonist activity at human BRS3
18
Total Activities
18
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
Synthesis and SAR of heterocyclic carboxylic acid isosteres 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 | 18 | 7.13 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088410 | — | — | 1 | 7.82 |
| CHEMBL1088409 | — | — | 1 | 7.62 |
| CHEMBL1089721 | — | — | 1 | 7.60 |
| CHEMBL1087443 | — | — | 1 | 7.54 |
| CHEMBL1094054 | — | — | 1 | 7.52 |
| CHEMBL1086672 | — | — | 1 | 7.39 |
| CHEMBL1088553 | — | — | 1 | 7.38 |
| CHEMBL1088411 | — | — | 1 | 7.38 |
| CHEMBL1088686 | — | — | 1 | 7.27 |
| CHEMBL1099034 | — | — | 1 | 7.25 |
| CHEMBL1087200 | — | — | 1 | 7.25 |
| CHEMBL1086674 | — | — | 1 | 7.11 |
| CHEMBL1087066 | — | — | 1 | 6.89 |
| CHEMBL1088684 | — | — | 1 | 6.88 |
| CHEMBL1086673 | — | — | 1 | 6.76 |
| CHEMBL1086684 | — | — | 1 | 6.47 |
| CHEMBL1087442 | — | — | 1 | 6.40 |
| CHEMBL1088685 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088410 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1088409 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1089721 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1087443 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1094054 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1086672 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1088553 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1088411 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1088686 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1099034 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1087200 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1086674 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1087066 | — | EC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1088684 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL1086673 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL1086684 | — | EC50 | = | 336.0 | nM | 6.47 |
| CHEMBL1087442 | — | EC50 | = | 399.0 | nM | 6.40 |
| CHEMBL1088685 | — | EC50 | = | 1767.0 | nM | 5.75 |