Assay Detail
Functional
CHEMBL926599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
37
Total Activities
37
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 | Intermediate |
Publication
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 7.57 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181076 | — | — | 1 | 8.50 |
| CHEMBL76781 | — | — | 1 | 8.40 |
| CHEMBL178366 | — | — | 1 | 8.40 |
| CHEMBL253591 | — | — | 1 | 8.40 |
| CHEMBL253807 | — | — | 1 | 8.40 |
| CHEMBL178124 | — | — | 1 | 8.20 |
| CHEMBL400600 | — | — | 1 | 8.20 |
| CHEMBL360492 | — | — | 1 | 8.20 |
| CHEMBL253806 | — | — | 1 | 8.10 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 8.10 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 8.10 |
| CHEMBL253805 | — | — | 1 | 8.10 |
| CHEMBL181787 | — | — | 1 | 8.10 |
| CHEMBL254009 | — | — | 1 | 8.10 |
| CHEMBL178231 | — | — | 1 | 8.10 |
| CHEMBL254215 | — | — | 1 | 8.00 |
| CHEMBL440752 | — | — | 1 | 8.00 |
| CHEMBL181172 | — | — | 1 | 7.90 |
| CHEMBL180668 | — | — | 1 | 7.90 |
| CHEMBL178365 | — | — | 1 | 7.80 |
| CHEMBL368016 | — | — | 1 | 7.70 |
| CHEMBL179337 | — | — | 1 | 7.70 |
| CHEMBL253810 | — | — | 1 | 7.70 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.60 |
| CHEMBL181672 | — | — | 1 | 7.60 |
| CHEMBL253811 | NORDEXFENFLURAMINE | — | 1 | 7.60 |
| CHEMBL253809 | — | — | 1 | 7.40 |
| CHEMBL399750 | — | — | 1 | 7.30 |
| CHEMBL361742 | — | — | 1 | 6.70 |
| CHEMBL398926 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181076 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL76781 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL253807 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL253591 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL178366 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL178124 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL400600 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL360492 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL253806 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL253805 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL181787 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL254009 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL178231 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL254215 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL440752 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL180668 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL181172 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL178365 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL368016 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL179337 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL253810 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL39 | SEROTONIN | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL181672 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL253811 | NORDEXFENFLURAMINE | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL253809 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL399750 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL361742 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL398926 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL178566 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL367796 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL178252 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL360479 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL362073 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL181324 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL253155 | — | EC50 | = | 3162.28 | nM | 5.50 |