Assay Detail
Binding
CHEMBL882495
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Inhibition of radioligand [3H]OT binding to oxytocin receptor (OT) in guinea pig myometrium membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Myometrium |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 7.72 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274397 | — | — | 1 | 8.22 |
| CHEMBL395429 | OXYTOCIN | 4.0 | 1 | 8.17 |
| CHEMBL265017 | — | — | 1 | 8.15 |
| CHEMBL414582 | — | — | 1 | 8.10 |
| CHEMBL87636 | — | — | 1 | 8.10 |
| CHEMBL411420 | — | — | 1 | 7.82 |
| CHEMBL330022 | — | — | 1 | 7.75 |
| CHEMBL438387 | — | — | 1 | 7.68 |
| CHEMBL415230 | — | — | 1 | 7.57 |
| CHEMBL384292 | — | — | 1 | 6.80 |
| CHEMBL1793955 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274397 | — | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL395429 | OXYTOCIN | Kd | = | 6.7 | nM | 8.17 |
| CHEMBL265017 | — | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL414582 | — | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL87636 | — | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL411420 | — | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL330022 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL438387 | — | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL415230 | — | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL384292 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL1793955 | — | Kd | = | 265.0 | nM | 6.58 |