Assay Detail
Binding
CHEMBL3377329
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Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 7.56 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3115400 | — | — | 1 | 9.00 |
| CHEMBL3115399 | — | — | 1 | 8.57 |
| CHEMBL3115388 | — | — | 1 | 8.57 |
| CHEMBL3115373 | — | — | 1 | 8.55 |
| CHEMBL3115386 | — | — | 1 | 8.47 |
| CHEMBL3115390 | — | — | 1 | 8.46 |
| CHEMBL3356412 | — | — | 1 | 8.43 |
| CHEMBL3356410 | — | — | 1 | 8.27 |
| CHEMBL3356411 | — | — | 1 | 8.25 |
| CHEMBL3356413 | — | — | 1 | 8.09 |
| CHEMBL3115395 | — | — | 1 | 7.91 |
| CHEMBL3115385 | — | — | 1 | 7.82 |
| CHEMBL3356407 | — | — | 1 | 7.70 |
| CHEMBL1672354 | — | — | 1 | 7.68 |
| CHEMBL2164575 | — | — | 1 | 7.48 |
| CHEMBL3115369 | — | — | 1 | 7.47 |
| CHEMBL3356405 | — | — | 1 | 7.46 |
| CHEMBL3356404 | — | — | 1 | 7.37 |
| CHEMBL3356409 | — | — | 1 | 7.35 |
| CHEMBL3115394 | — | — | 1 | 7.34 |
| CHEMBL3115377 | — | — | 1 | 7.28 |
| CHEMBL3115389 | — | — | 1 | 7.21 |
| CHEMBL3115378 | — | — | 1 | 7.21 |
| CHEMBL3356406 | — | — | 1 | 7.09 |
| CHEMBL3115379 | — | — | 1 | 6.92 |
| CHEMBL2023109 | — | — | 1 | 6.89 |
| CHEMBL3115392 | — | — | 1 | 6.64 |
| CHEMBL3115370 | — | — | 1 | 6.59 |
| CHEMBL3356403 | — | — | 1 | 6.55 |
| CHEMBL3115376 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3115400 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3115399 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3115388 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3115373 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3115386 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3115390 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3356412 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3356410 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3356411 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3356413 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3115395 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL3115385 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3356407 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1672354 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2164575 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3115369 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3356405 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3356404 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3356409 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3115394 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3115377 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3115389 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3115378 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3356406 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3115379 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2023109 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3115392 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3115370 | — | EC50 | = | 256.0 | nM | 6.59 |
| CHEMBL3356403 | — | EC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3115376 | — | EC50 | = | 569.0 | nM | 6.25 |
| CHEMBL3115387 | — | EC50 | = | 3124.0 | nM | 5.50 |
| CHEMBL3356402 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3356408 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3115393 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3115391 | — | EC50 | > | 10000.0 | nM | - |