Assay Detail
Binding
CHEMBL3756314
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]mesulergine from 5HT2C in Sprague-Dawley rat whole brain membranes after 1 hr by liquid scintillation spectrometry
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.99 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | — | 1 | 9.80 |
| CHEMBL3752465 | — | — | 1 | 9.22 |
| CHEMBL3261693 | — | — | 1 | 8.52 |
| CHEMBL3753329 | — | — | 1 | 8.35 |
| CHEMBL3754784 | — | — | 1 | 8.21 |
| CHEMBL3753681 | — | — | 1 | 8.09 |
| CHEMBL3261690 | — | — | 1 | 7.97 |
| CHEMBL3261695 | — | — | 1 | 7.95 |
| CHEMBL3753894 | — | — | 1 | 7.94 |
| CHEMBL3752844 | — | — | 1 | 7.84 |
| CHEMBL3261686 | — | — | 1 | 7.80 |
| CHEMBL3754137 | — | — | 1 | 7.79 |
| CHEMBL3753516 | — | — | 1 | 7.58 |
| CHEMBL3753075 | — | — | 1 | 7.36 |
| CHEMBL3752059 | — | — | 1 | 7.02 |
| CHEMBL3753283 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL3752465 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3261693 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3753329 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3754784 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3753681 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL3261690 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL3261695 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL3753894 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL3752844 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL3261686 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL3754137 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL3753516 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL3753075 | — | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL3752059 | — | Ki | = | 95.6 | nM | 7.02 |
| CHEMBL3753283 | — | Ki | = | 477.0 | nM | 6.32 |