Assay Detail
Binding
CHEMBL4681104
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Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Discovery of Functionally Selective Serotonin 2C (5-HT) Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.31 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331803 | — | — | 2 | 8.00 |
| CHEMBL4790992 | — | — | 2 | 7.71 |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 7.68 |
| CHEMBL4779260 | — | — | 2 | 7.60 |
| CHEMBL4781163 | — | — | 2 | 7.52 |
| CHEMBL360328 | LORCASERIN | 4.0 | 2 | 7.23 |
| CHEMBL4761064 | — | — | 2 | 7.02 |
| CHEMBL4743977 | — | — | 2 | 6.57 |
| CHEMBL4752976 | — | — | 2 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331803 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2331803 | — | EC50 | = | 10.72 | nM | 7.97 |
| CHEMBL4790992 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4790992 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL39 | SEROTONIN | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL39 | SEROTONIN | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL4779260 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4779260 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4781163 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4781163 | — | EC50 | = | 30.2 | nM | 7.52 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4761064 | — | EC50 | = | 95.5 | nM | 7.02 |
| CHEMBL4761064 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4743977 | — | EC50 | = | 267.0 | nM | 6.57 |
| CHEMBL4743977 | — | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL4752976 | — | EC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4752976 | — | EC50 | = | 323.59 | nM | 6.49 |