Assay Detail
Binding
CHEMBL885138
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Displacement of [3H]oxytocin from human Oxytocin receptor
32
Total Activities
32
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. 2. Synthesis, chirality, and pharmacokinetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.73 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371008 | — | — | 1 | 8.80 |
| CHEMBL372615 | — | — | 1 | 8.70 |
| CHEMBL372554 | — | — | 1 | 8.70 |
| CHEMBL372128 | — | — | 1 | 8.60 |
| CHEMBL381024 | — | — | 1 | 8.60 |
| CHEMBL196603 | — | — | 1 | 8.50 |
| CHEMBL382518 | — | — | 1 | 8.40 |
| CHEMBL372978 | — | — | 1 | 8.40 |
| CHEMBL555148 | — | — | 1 | 8.40 |
| CHEMBL197793 | — | — | 1 | 8.40 |
| CHEMBL196780 | — | — | 1 | 8.30 |
| CHEMBL198329 | — | — | 1 | 8.30 |
| CHEMBL194374 | — | — | 1 | 8.30 |
| CHEMBL193773 | — | — | 1 | 8.20 |
| CHEMBL194584 | — | — | 1 | 8.00 |
| CHEMBL382065 | — | — | 1 | 7.60 |
| CHEMBL371291 | — | — | 1 | 7.60 |
| CHEMBL197298 | — | — | 1 | 7.50 |
| CHEMBL197822 | — | — | 1 | 7.40 |
| CHEMBL273988 | — | — | 1 | 7.30 |
| CHEMBL194922 | — | — | 1 | 7.30 |
| CHEMBL194432 | — | — | 1 | 7.20 |
| CHEMBL194233 | — | — | 1 | 7.10 |
| CHEMBL198328 | — | — | 1 | 7.10 |
| CHEMBL197833 | — | — | 1 | 7.00 |
| CHEMBL427353 | — | — | 1 | 7.00 |
| CHEMBL372619 | — | — | 1 | 6.90 |
| CHEMBL196688 | — | — | 1 | 6.80 |
| CHEMBL198964 | — | — | 1 | 6.80 |
| CHEMBL372516 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371008 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL372615 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL372554 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL372128 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL381024 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL196603 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL382518 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL372978 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL555148 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL197793 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL196780 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL198329 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL194374 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL193773 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL194584 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL371291 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL382065 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL197298 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL197822 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL273988 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL194922 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL194432 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL194233 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL198328 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL197833 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL427353 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL372619 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL196688 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL198964 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL372516 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL371983 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL194431 | — | Ki | = | 316.23 | nM | 6.50 |