Assay Detail
Binding
CHEMBL4325227
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Agonist activity at recombinant human Gi/Go-coupled OTR expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins in presence of 10% FBS by pathhunter assay
14
Total Activities
14
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
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.50 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL395429 | OXYTOCIN | 4.0 | 1 | 8.64 |
| CHEMBL3301668 | CARBETOCIN | 3.0 | 1 | 8.52 |
| CHEMBL4460622 | — | — | 1 | 8.32 |
| CHEMBL4463103 | — | — | 1 | 8.28 |
| CHEMBL4550811 | — | — | 1 | 7.84 |
| CHEMBL4546106 | — | — | 1 | 7.72 |
| CHEMBL4442222 | — | — | 1 | 7.25 |
| CHEMBL4546597 | — | — | 1 | 6.76 |
| CHEMBL4537162 | — | — | 1 | 6.71 |
| CHEMBL4456573 | — | — | 1 | 6.33 |
| CHEMBL4560445 | — | — | 1 | 6.08 |
| CHEMBL4541779 | — | — | 1 | - |
| CHEMBL4589487 | — | — | 1 | - |
| CHEMBL4532581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL395429 | OXYTOCIN | EC50 | = | 2.29 | nM | 8.64 |
| CHEMBL3301668 | CARBETOCIN | EC50 | = | 2.99 | nM | 8.52 |
| CHEMBL4460622 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4463103 | — | EC50 | = | 5.28 | nM | 8.28 |
| CHEMBL4550811 | — | EC50 | = | 14.42 | nM | 7.84 |
| CHEMBL4546106 | — | EC50 | = | 18.93 | nM | 7.72 |
| CHEMBL4442222 | — | EC50 | = | 56.94 | nM | 7.25 |
| CHEMBL4546597 | — | EC50 | = | 173.4 | nM | 6.76 |
| CHEMBL4537162 | — | EC50 | = | 192.6 | nM | 6.71 |
| CHEMBL4456573 | — | EC50 | = | 463.8 | nM | 6.33 |
| CHEMBL4560445 | — | EC50 | = | 831.2 | nM | 6.08 |
| CHEMBL4541779 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4589487 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4532581 | — | EC50 | > | 1000.0 | nM | - |