Assay Detail
Binding
CHEMBL617280
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Binding affinity using [3H]mesulergine as radioligand with receptor membranes isolated from a CHO-k cell line expressing the human 5-hydroxytryptamine 2C receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-k |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.62 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58009 | — | — | 1 | 7.75 |
| CHEMBL303516 | — | — | 1 | 7.50 |
| CHEMBL301466 | — | — | 1 | 7.24 |
| CHEMBL61695 | — | — | 1 | 7.21 |
| CHEMBL304013 | — | — | 1 | 7.08 |
| CHEMBL291794 | — | — | 1 | 7.06 |
| CHEMBL305123 | — | — | 1 | 7.04 |
| CHEMBL60280 | — | — | 1 | 6.80 |
| CHEMBL59631 | — | — | 1 | 6.62 |
| CHEMBL60830 | — | — | 1 | 6.54 |
| CHEMBL61771 | — | — | 1 | 6.43 |
| CHEMBL59620 | — | — | 1 | 5.77 |
| CHEMBL59807 | — | — | 1 | 5.75 |
| CHEMBL59619 | — | — | 1 | 5.44 |
| CHEMBL410512 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58009 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL303516 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL301466 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL61695 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL304013 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL291794 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL305123 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL60280 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL59631 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL60830 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL61771 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL59620 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL59807 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL59619 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL410512 | — | Ki | = | 9200.0 | nM | 5.04 |