Assay Detail
Functional
CHEMBL1067826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant 5HT2C receptor expressed in HEK293E cells by FLIPR assay
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 7.31 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL590483 | — | — | 1 | 8.74 |
| CHEMBL590580 | — | — | 1 | 8.70 |
| CHEMBL590531 | — | — | 2 | 8.18 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.82 |
| CHEMBL590816 | — | — | 1 | 7.80 |
| CHEMBL590331 | — | — | 1 | 7.47 |
| CHEMBL605402 | — | — | 1 | 7.37 |
| CHEMBL590078 | — | — | 2 | 7.35 |
| CHEMBL590333 | — | — | 1 | 7.04 |
| CHEMBL590482 | — | — | 1 | 6.96 |
| CHEMBL590089 | — | — | 1 | 6.88 |
| CHEMBL590077 | — | — | 1 | 6.86 |
| CHEMBL590332 | — | — | 1 | 5.38 |
| CHEMBL603527 | — | — | 1 | - |
| CHEMBL590721 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL590483 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL590580 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL590531 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL590816 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL590331 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL605402 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL590078 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL590333 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL590531 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL590482 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL590089 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL590077 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL590078 | — | EC50 | = | 989.0 | nM | 6.00 |
| CHEMBL590332 | — | EC50 | = | 4197.0 | nM | 5.38 |
| CHEMBL603527 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL590721 | — | EC50 | - | — | - |