Assay Detail
Binding
CHEMBL1110001
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human BRS3
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 18 | 7.64 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094054 | — | — | 1 | 8.28 |
| CHEMBL1088409 | — | — | 1 | 8.28 |
| CHEMBL1088410 | — | — | 1 | 8.21 |
| CHEMBL1086672 | — | — | 1 | 8.21 |
| CHEMBL1087443 | — | — | 1 | 8.00 |
| CHEMBL1089721 | — | — | 1 | 7.96 |
| CHEMBL1099034 | — | — | 1 | 7.82 |
| CHEMBL1088553 | — | — | 1 | 7.75 |
| CHEMBL1087200 | — | — | 1 | 7.70 |
| CHEMBL1086673 | — | — | 1 | 7.66 |
| CHEMBL1088411 | — | — | 1 | 7.58 |
| CHEMBL1086674 | — | — | 1 | 7.57 |
| CHEMBL1086684 | — | — | 1 | 7.51 |
| CHEMBL1088684 | — | — | 1 | 7.51 |
| CHEMBL1087442 | — | — | 1 | 7.08 |
| CHEMBL1088686 | — | — | 1 | 6.99 |
| CHEMBL1087066 | — | — | 1 | 6.90 |
| CHEMBL1088685 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094054 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1088409 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1088410 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1086672 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1087443 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1089721 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1099034 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1088553 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1087200 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1086673 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1088411 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1086674 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1086684 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1088684 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1087442 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1088686 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1087066 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL1088685 | — | IC50 | = | 287.0 | nM | 6.54 |