Assay Detail
Binding
CHEMBL4427988
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Agonist activity at mouse BRS3 expressed in CHOK1 cells measured after 1 hrs by IP-One HTRF assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel imidazol-1-ylacetic acid derivatives as non-brain penetrant bombesin receptor subtype-3 (BRS-3) agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 7.29 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4435571 | — | — | 1 | 9.10 |
| CHEMBL4580739 | — | — | 1 | 8.70 |
| CHEMBL4461212 | — | — | 1 | 8.52 |
| CHEMBL4448589 | — | — | 1 | 8.40 |
| CHEMBL4593256 | — | — | 1 | 8.30 |
| CHEMBL4464287 | — | — | 1 | 8.15 |
| CHEMBL4522752 | — | — | 1 | 7.89 |
| CHEMBL4482945 | — | — | 1 | 7.62 |
| CHEMBL4557722 | — | — | 1 | 7.60 |
| CHEMBL4449347 | — | — | 1 | 7.58 |
| CHEMBL4514194 | — | — | 1 | 7.36 |
| CHEMBL4451347 | — | — | 1 | 7.21 |
| CHEMBL4476111 | — | — | 1 | 6.85 |
| CHEMBL4544477 | — | — | 1 | 6.30 |
| CHEMBL4442362 | — | — | 1 | 6.21 |
| CHEMBL4522974 | — | — | 1 | 6.16 |
| CHEMBL4590481 | — | — | 1 | 5.90 |
| CHEMBL4518142 | — | — | 1 | 5.72 |
| CHEMBL4448645 | — | — | 1 | 5.00 |
| CHEMBL4585527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4435571 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4580739 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4461212 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4448589 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4593256 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4464287 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4522752 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4482945 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4557722 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4449347 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4514194 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4451347 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4476111 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4544477 | — | EC50 | = | 498.0 | nM | 6.30 |
| CHEMBL4442362 | — | EC50 | = | 621.0 | nM | 6.21 |
| CHEMBL4522974 | — | EC50 | = | 694.0 | nM | 6.16 |
| CHEMBL4590481 | — | EC50 | = | 1271.0 | nM | 5.90 |
| CHEMBL4518142 | — | EC50 | = | 1906.0 | nM | 5.72 |
| CHEMBL4448645 | — | EC50 | = | 9908.0 | nM | 5.00 |
| CHEMBL4585527 | — | EC50 | > | 10000.0 | nM | - |