Assay Detail
Functional
CHEMBL837403
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration towards 5-hydroxytryptamine 2A 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 | 6.82 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL178366 | — | — | 1 | 7.80 |
| CHEMBL179244 | — | — | 1 | 7.66 |
| CHEMBL182184 | — | — | 1 | 7.52 |
| CHEMBL179915 | — | — | 1 | 7.38 |
| CHEMBL179378 | — | — | 1 | 7.21 |
| CHEMBL178313 | — | — | 1 | 7.20 |
| CHEMBL360492 | — | — | 1 | 7.14 |
| CHEMBL180867 | — | — | 1 | 7.10 |
| CHEMBL180815 | — | — | 1 | 7.10 |
| CHEMBL181787 | — | — | 1 | 7.10 |
| CHEMBL180668 | — | — | 1 | 7.05 |
| CHEMBL415029 | — | — | 1 | 7.01 |
| CHEMBL178124 | — | — | 1 | 7.00 |
| CHEMBL426235 | — | — | 1 | 7.00 |
| CHEMBL180166 | — | — | 1 | 7.00 |
| CHEMBL360968 | — | — | 1 | 6.96 |
| CHEMBL181076 | — | — | 1 | 6.87 |
| CHEMBL181672 | — | — | 1 | 6.82 |
| CHEMBL179337 | — | — | 1 | 6.77 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 6.72 |
| CHEMBL178231 | — | — | 1 | 6.66 |
| CHEMBL178365 | — | — | 1 | 6.58 |
| CHEMBL181172 | — | — | 1 | 6.58 |
| CHEMBL440752 | — | — | 1 | 6.29 |
| CHEMBL368016 | — | — | 1 | 6.08 |
| CHEMBL361742 | — | — | 1 | 6.03 |
| CHEMBL367796 | — | — | 1 | 5.80 |
| CHEMBL178252 | — | — | 1 | 5.80 |
| CHEMBL178566 | — | — | 1 | 5.62 |
| CHEMBL179329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL178366 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL179244 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL182184 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL179915 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL179378 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL178313 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL360492 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL180867 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL180815 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL181787 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL180668 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL415029 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL178124 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL426235 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL180166 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL360968 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL181076 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL181672 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL179337 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL178231 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL178365 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL181172 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL440752 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL368016 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL361742 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL367796 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL178252 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL178566 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL179329 | — | EC50 | - | nM | - | |
| CHEMBL181324 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL362073 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL360479 | — | EC50 | > | 5000.0 | nM | - |