Assay Detail
Binding
CHEMBL2445945
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in Flp-IN HEK cells
45
Total Activities
45
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
In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 45 | 5.75 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2442272 | — | — | 1 | 7.46 |
| CHEMBL2058703 | — | — | 1 | 7.10 |
| CHEMBL2442273 | — | — | 1 | 6.70 |
| CHEMBL2058415 | — | — | 1 | 6.50 |
| CHEMBL2442270 | — | — | 1 | 6.46 |
| CHEMBL2058704 | — | — | 1 | 6.37 |
| CHEMBL2442271 | — | — | 1 | 6.22 |
| CHEMBL2058706 | — | — | 1 | 6.17 |
| CHEMBL2442274 | — | — | 1 | 6.08 |
| CHEMBL2058698 | — | — | 1 | 6.05 |
| CHEMBL2058702 | — | — | 1 | 6.01 |
| CHEMBL2058705 | — | — | 1 | 6.01 |
| CHEMBL2058416 | — | — | 1 | 5.97 |
| CHEMBL2058428 | — | — | 1 | 5.91 |
| CHEMBL2442276 | — | — | 1 | 5.90 |
| CHEMBL1170237 | — | — | 1 | 5.90 |
| CHEMBL2442267 | — | — | 1 | 5.87 |
| CHEMBL2442275 | — | — | 1 | 5.77 |
| CHEMBL463249 | — | — | 1 | 5.77 |
| CHEMBL2058426 | — | — | 1 | 5.73 |
| CHEMBL2058694 | — | — | 1 | 5.73 |
| CHEMBL511879 | — | — | 1 | 5.72 |
| CHEMBL2058407 | — | — | 1 | 5.70 |
| CHEMBL2058699 | — | — | 1 | 5.68 |
| CHEMBL2058418 | — | — | 1 | 5.66 |
| CHEMBL2058417 | — | — | 1 | 5.64 |
| CHEMBL2442266 | — | — | 1 | 5.63 |
| CHEMBL508657 | ISOPLYSIN A | — | 1 | 5.63 |
| CHEMBL2058427 | — | — | 1 | 5.61 |
| CHEMBL1173331 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2442272 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2058703 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2442273 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL2058415 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2442270 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL2058704 | — | Ki | = | 426.0 | nM | 6.37 |
| CHEMBL2442271 | — | Ki | = | 604.0 | nM | 6.22 |
| CHEMBL2058706 | — | Ki | = | 678.0 | nM | 6.17 |
| CHEMBL2442274 | — | Ki | = | 841.0 | nM | 6.08 |
| CHEMBL2058698 | — | Ki | = | 885.0 | nM | 6.05 |
| CHEMBL2058702 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL2058705 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL2058416 | — | Ki | = | 1078.0 | nM | 5.97 |
| CHEMBL2058428 | — | Ki | = | 1239.0 | nM | 5.91 |
| CHEMBL1170237 | — | Ki | = | 1265.0 | nM | 5.90 |
| CHEMBL2442276 | — | Ki | = | 1271.0 | nM | 5.90 |
| CHEMBL2442267 | — | Ki | = | 1343.0 | nM | 5.87 |
| CHEMBL2442275 | — | Ki | = | 1698.0 | nM | 5.77 |
| CHEMBL463249 | — | Ki | = | 1704.0 | nM | 5.77 |
| CHEMBL2058426 | — | Ki | = | 1856.0 | nM | 5.73 |
| CHEMBL2058694 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL511879 | — | Ki | = | 1916.0 | nM | 5.72 |
| CHEMBL2058407 | — | Ki | = | 2013.0 | nM | 5.70 |
| CHEMBL2058699 | — | Ki | = | 2094.0 | nM | 5.68 |
| CHEMBL2058418 | — | Ki | = | 2208.0 | nM | 5.66 |
| CHEMBL2058417 | — | Ki | = | 2275.0 | nM | 5.64 |
| CHEMBL2442266 | — | Ki | = | 2339.0 | nM | 5.63 |
| CHEMBL508657 | ISOPLYSIN A | Ki | = | 2354.0 | nM | 5.63 |
| CHEMBL2058427 | — | Ki | = | 2430.0 | nM | 5.61 |
| CHEMBL1173331 | — | Ki | = | 2454.0 | nM | 5.61 |
| CHEMBL2058419 | — | Ki | = | 2762.0 | nM | 5.56 |
| CHEMBL2058420 | — | Ki | = | 3013.0 | nM | 5.52 |
| CHEMBL2058408 | — | Ki | = | 3883.0 | nM | 5.41 |
| CHEMBL2058409 | — | Ki | = | 4129.0 | nM | 5.38 |
| CHEMBL2058695 | — | Ki | = | 4348.0 | nM | 5.36 |
| CHEMBL2058700 | — | Ki | = | 4367.0 | nM | 5.36 |
| CHEMBL1173525 | — | Ki | = | 4778.0 | nM | 5.32 |
| CHEMBL2058429 | — | Ki | = | 6470.0 | nM | 5.19 |
| CHEMBL512332 | METHYLAPLYSINOPSIN | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL513803 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL2442277 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL404232 | APLYSINOPSIN | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL2442265 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL2442268 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL2442269 | — | Ki | = | 10000.0 | nM | 5.00 |