Assay Detail
Binding
CHEMBL3377328
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Agonist activity at human 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 | Homo sapiens |
| 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 | 7.63 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3115400 | — | — | 1 | 8.89 |
| CHEMBL3115386 | — | — | 1 | 8.80 |
| CHEMBL3115390 | — | — | 1 | 8.77 |
| CHEMBL3115388 | — | — | 1 | 8.77 |
| CHEMBL3356412 | — | — | 1 | 8.47 |
| CHEMBL3115399 | — | — | 1 | 8.44 |
| CHEMBL3356411 | — | — | 1 | 8.40 |
| CHEMBL3356410 | — | — | 1 | 8.38 |
| CHEMBL3356413 | — | — | 1 | 8.25 |
| CHEMBL3115395 | — | — | 1 | 8.07 |
| CHEMBL3356407 | — | — | 1 | 8.06 |
| CHEMBL3115373 | — | — | 1 | 8.02 |
| CHEMBL3356404 | — | — | 1 | 7.92 |
| CHEMBL3115385 | — | — | 1 | 7.89 |
| CHEMBL1672354 | — | — | 1 | 7.85 |
| CHEMBL3115389 | — | — | 1 | 7.77 |
| CHEMBL3356405 | — | — | 1 | 7.72 |
| CHEMBL3115394 | — | — | 1 | 7.60 |
| CHEMBL3356409 | — | — | 1 | 7.40 |
| CHEMBL3356406 | — | — | 1 | 7.38 |
| CHEMBL3115392 | — | — | 1 | 7.32 |
| CHEMBL3115377 | — | — | 1 | 7.23 |
| CHEMBL3356403 | — | — | 1 | 7.17 |
| CHEMBL3115378 | — | — | 1 | 7.16 |
| CHEMBL2023109 | — | — | 1 | 7.14 |
| CHEMBL2164575 | — | — | 1 | 7.01 |
| CHEMBL3115369 | — | — | 1 | 6.88 |
| CHEMBL3115379 | — | — | 1 | 6.70 |
| CHEMBL3115393 | — | — | 1 | 6.43 |
| CHEMBL3115376 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3115400 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3115386 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3115390 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3115388 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3356412 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3115399 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3356411 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3356410 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3356413 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3115395 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3356407 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3115373 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3356404 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3115385 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1672354 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3115389 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3356405 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3115394 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3356409 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3356406 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3115392 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3115377 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3356403 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3115378 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2023109 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2164575 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3115369 | — | EC50 | = | 131.0 | nM | 6.88 |
| CHEMBL3115379 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3115393 | — | EC50 | = | 368.0 | nM | 6.43 |
| CHEMBL3115376 | — | EC50 | = | 381.0 | nM | 6.42 |
| CHEMBL3115370 | — | EC50 | = | 916.0 | nM | 6.04 |
| CHEMBL3115387 | — | EC50 | = | 2071.0 | nM | 5.68 |
| CHEMBL3356408 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3356402 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3115391 | — | EC50 | > | 10000.0 | nM | - |