Assay Detail
Functional
CHEMBL2027396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human BRS3 expressed in human HEK293AEQ cells measured for 10 mins by aequorin bioluminescence assay
6
Total Activities
6
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
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.42 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2023114 | — | — | 1 | 7.82 |
| CHEMBL2023113 | — | — | 1 | 7.68 |
| CHEMBL2023112 | — | — | 1 | 7.58 |
| CHEMBL2023110 | — | — | 1 | 7.19 |
| CHEMBL2023109 | — | — | 1 | 7.14 |
| CHEMBL2023111 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2023114 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2023113 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2023112 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2023110 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2023109 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2023111 | — | EC50 | = | 82.0 | nM | 7.09 |