Assay Detail
Functional
CHEMBL837404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release
32
Total Activities
32
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 | 32 | 6.49 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182184 | — | — | 1 | 7.52 |
| CHEMBL426235 | — | — | 1 | 7.40 |
| CHEMBL179378 | — | — | 1 | 7.19 |
| CHEMBL178366 | — | — | 1 | 7.11 |
| CHEMBL180815 | — | — | 1 | 7.00 |
| CHEMBL179915 | — | — | 1 | 6.89 |
| CHEMBL181787 | — | — | 1 | 6.85 |
| CHEMBL360968 | — | — | 1 | 6.75 |
| CHEMBL178313 | — | — | 1 | 6.72 |
| CHEMBL180867 | — | — | 1 | 6.66 |
| CHEMBL415029 | — | — | 1 | 6.64 |
| CHEMBL360492 | — | — | 1 | 6.44 |
| CHEMBL178124 | — | — | 1 | 6.42 |
| CHEMBL180166 | — | — | 1 | 6.40 |
| CHEMBL181672 | — | — | 1 | 6.28 |
| CHEMBL361742 | — | — | 1 | 6.11 |
| CHEMBL179337 | — | — | 1 | 6.08 |
| CHEMBL179329 | — | — | 1 | 6.00 |
| CHEMBL180668 | — | — | 1 | 6.00 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 6.00 |
| CHEMBL181172 | — | — | 1 | 5.96 |
| CHEMBL178365 | — | — | 1 | 5.85 |
| CHEMBL440752 | — | — | 1 | 5.82 |
| CHEMBL178231 | — | — | 1 | 5.75 |
| CHEMBL368016 | — | — | 1 | - |
| CHEMBL179244 | — | — | 1 | - |
| CHEMBL181324 | — | — | 1 | - |
| CHEMBL367796 | — | — | 1 | - |
| CHEMBL362073 | — | — | 1 | - |
| CHEMBL360479 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182184 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL426235 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL179378 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL178366 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL180815 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL179915 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL181787 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL360968 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL178313 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL180867 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL415029 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL360492 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL178124 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL180166 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL181672 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL361742 | — | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL179337 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL179329 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL180668 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL181172 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL178365 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL440752 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL178231 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL368016 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL179244 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL181324 | — | EC50 | - | — | - | |
| CHEMBL367796 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL362073 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL360479 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL178252 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL178566 | — | EC50 | > | 10000.0 | nM | - |