Assay Detail
Binding
CHEMBL840223
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Mean negative logarithim of binding affinity was measured for the rat serotonin transporter; n>/=3
18
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.41 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113021 | — | — | 1 | 8.30 |
| CHEMBL180557 | — | — | 1 | 8.20 |
| CHEMBL183460 | — | — | 1 | 8.20 |
| CHEMBL3706797 | — | — | 1 | 8.10 |
| CHEMBL180405 | — | — | 1 | 7.60 |
| CHEMBL183332 | — | — | 1 | 7.50 |
| CHEMBL180182 | — | — | 1 | 7.50 |
| CHEMBL181186 | — | — | 1 | 7.40 |
| CHEMBL183921 | — | — | 5 | 7.30 |
| CHEMBL183034 | — | — | 1 | 7.30 |
| CHEMBL183551 | — | — | 1 | 7.30 |
| CHEMBL180700 | — | — | 1 | 7.10 |
| CHEMBL183901 | — | — | 1 | 7.10 |
| CHEMBL180445 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113021 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL183460 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL180557 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL3706797 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL180405 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL183332 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL180182 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL181186 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL183551 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL183921 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL183034 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL183901 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL180700 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL183921 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL183921 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL180445 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL183921 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL183921 | — | Ki | = | 316.23 | nM | 6.50 |