Assay Detail
Binding
CHEMBL870934
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Displacement of [3H]oxytocin from human OTR
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.82 | 9.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL210029 | — | — | 1 | 9.90 |
| CHEMBL379192 | — | — | 1 | 9.40 |
| CHEMBL438609 | — | — | 1 | 9.30 |
| CHEMBL211556 | — | — | 1 | 9.20 |
| CHEMBL377315 | — | — | 1 | 9.20 |
| CHEMBL377414 | — | — | 1 | 9.20 |
| CHEMBL378718 | — | — | 1 | 9.20 |
| CHEMBL208787 | — | — | 1 | 9.00 |
| CHEMBL211443 | — | — | 1 | 8.90 |
| CHEMBL196478 | — | — | 1 | 8.90 |
| CHEMBL427227 | — | — | 1 | 8.80 |
| CHEMBL196603 | — | — | 1 | 8.50 |
| CHEMBL213112 | — | — | 1 | 8.40 |
| CHEMBL211440 | — | — | 1 | 8.40 |
| CHEMBL378939 | — | — | 1 | 8.40 |
| CHEMBL209917 | — | — | 1 | 7.90 |
| CHEMBL382301 | ATOSIBAN | 4.0 | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL210029 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL379192 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL438609 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL211556 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL377315 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL377414 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL378718 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL208787 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL211443 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL196478 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL427227 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL196603 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL213112 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL211440 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL378939 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL209917 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL382301 | ATOSIBAN | Ki | = | 39.81 | nM | 7.40 |