Assay Detail
Binding
CHEMBL938539
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Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.92 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490417 | — | — | 1 | 9.70 |
| CHEMBL484059 | — | — | 1 | 9.50 |
| CHEMBL444398 | — | — | 1 | 9.40 |
| CHEMBL496520 | — | — | 1 | 9.40 |
| CHEMBL521506 | — | — | 1 | 9.30 |
| CHEMBL522257 | — | — | 1 | 9.30 |
| CHEMBL497980 | — | — | 1 | 9.30 |
| CHEMBL491839 | — | — | 1 | 9.20 |
| CHEMBL484260 | — | — | 1 | 9.20 |
| CHEMBL489195 | — | — | 1 | 9.20 |
| CHEMBL489393 | — | — | 1 | 9.10 |
| CHEMBL490211 | — | — | 1 | 9.10 |
| CHEMBL523064 | — | — | 1 | 9.10 |
| CHEMBL489394 | — | — | 1 | 9.00 |
| CHEMBL495703 | — | — | 1 | 8.90 |
| CHEMBL496317 | — | — | 1 | 8.80 |
| CHEMBL495705 | — | — | 1 | 8.70 |
| CHEMBL485491 | — | — | 1 | 8.60 |
| CHEMBL521873 | — | — | 1 | 8.10 |
| CHEMBL523095 | — | — | 1 | 7.50 |
| CHEMBL497979 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490417 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL484059 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL444398 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL496520 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL521506 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL522257 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL497980 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL491839 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL484260 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL489195 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL489393 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL490211 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL523064 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL489394 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL495703 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL496317 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL495705 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL485491 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL521873 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL523095 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL497979 | — | Ki | = | 125.89 | nM | 6.90 |