Assay Detail
Functional
CHEMBL837402
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 7.61 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179378 | — | — | 1 | 8.70 |
| CHEMBL180867 | — | — | 1 | 8.52 |
| CHEMBL178313 | — | — | 1 | 8.52 |
| CHEMBL181076 | — | — | 1 | 8.52 |
| CHEMBL178366 | — | — | 1 | 8.40 |
| CHEMBL179915 | — | — | 1 | 8.40 |
| CHEMBL182184 | — | — | 1 | 8.30 |
| CHEMBL180815 | — | — | 1 | 8.30 |
| CHEMBL178231 | — | — | 1 | 8.22 |
| CHEMBL178124 | — | — | 1 | 8.15 |
| CHEMBL360492 | — | — | 1 | 8.15 |
| CHEMBL180166 | — | — | 1 | 8.10 |
| CHEMBL426235 | — | — | 1 | 7.96 |
| CHEMBL181787 | — | — | 1 | 7.96 |
| CHEMBL181172 | — | — | 1 | 7.96 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 7.96 |
| CHEMBL440752 | — | — | 1 | 7.92 |
| CHEMBL180668 | — | — | 1 | 7.92 |
| CHEMBL178365 | — | — | 1 | 7.80 |
| CHEMBL179337 | — | — | 1 | 7.70 |
| CHEMBL368016 | — | — | 1 | 7.66 |
| CHEMBL360968 | — | — | 1 | 7.55 |
| CHEMBL181672 | — | — | 1 | 7.46 |
| CHEMBL179244 | — | — | 1 | 7.25 |
| CHEMBL415029 | — | — | 1 | 7.17 |
| CHEMBL179329 | — | — | 1 | 6.80 |
| CHEMBL178566 | — | — | 1 | 6.64 |
| CHEMBL367796 | — | — | 1 | 6.47 |
| CHEMBL178252 | — | — | 1 | 6.39 |
| CHEMBL361742 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179378 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL180867 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL181076 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL178313 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL178366 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL179915 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL182184 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL180815 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL178231 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL178124 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL360492 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL180166 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL181172 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL181787 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL426235 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL440752 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL180668 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL178365 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL179337 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL368016 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL360968 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL181672 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL179244 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL415029 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL179329 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL178566 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL367796 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL178252 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL361742 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL362073 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL360479 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL181324 | — | EC50 | = | 2000.0 | nM | 5.70 |