Assay Detail
Binding
CHEMBL4714288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-DOI from recombinant human 5HT2CR transfected in human HEK293 cells incubated for 45 mins by radioligand binding assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.09 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4765074 | — | — | 1 | 9.80 |
| CHEMBL4213379 | — | — | 1 | 9.60 |
| CHEMBL4776557 | — | — | 1 | 9.50 |
| CHEMBL4213447 | — | — | 1 | 9.30 |
| CHEMBL4778570 | — | — | 1 | 9.30 |
| CHEMBL4777852 | — | — | 1 | 9.20 |
| CHEMBL4206126 | — | — | 1 | 8.80 |
| CHEMBL4757718 | — | — | 1 | 8.70 |
| CHEMBL4218374 | — | — | 1 | 8.70 |
| CHEMBL4785566 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4765074 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL4213379 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL4776557 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL4213447 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL4778570 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL4777852 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL4206126 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL4757718 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4218374 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4785566 | — | Ki | = | 10.0 | nM | 8.00 |