Assay Detail
Functional
CHEMBL3419957
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Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
27
Total Activities
27
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 | Autocuration |
Publication
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 5.79 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 9.04 |
| CHEMBL3416033 | — | — | 1 | 7.07 |
| CHEMBL3416053 | — | — | 1 | 6.38 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 6.32 |
| CHEMBL3416055 | — | — | 1 | 6.20 |
| CHEMBL3416060 | — | — | 1 | 6.13 |
| CHEMBL3416057 | — | — | 1 | 6.08 |
| CHEMBL3416039 | — | — | 1 | 6.00 |
| CHEMBL3416056 | — | — | 1 | 5.83 |
| CHEMBL3416051 | — | — | 1 | 5.77 |
| CHEMBL3416061 | — | — | 1 | 5.70 |
| CHEMBL3416047 | — | — | 1 | 5.66 |
| CHEMBL3416032 | — | — | 1 | 5.64 |
| CHEMBL3416040 | — | — | 1 | 5.52 |
| CHEMBL3416034 | — | — | 1 | 5.52 |
| CHEMBL3416035 | — | — | 1 | 5.46 |
| CHEMBL3416046 | — | — | 1 | 5.37 |
| CHEMBL3416048 | — | — | 1 | 5.36 |
| CHEMBL3416049 | — | — | 1 | 5.34 |
| CHEMBL3416054 | — | — | 1 | 5.34 |
| CHEMBL3416059 | — | — | 1 | 5.31 |
| CHEMBL3416041 | — | — | 1 | 5.30 |
| CHEMBL3416042 | — | — | 1 | 5.28 |
| CHEMBL3416038 | — | — | 1 | 5.25 |
| CHEMBL3416052 | — | — | 1 | 5.21 |
| CHEMBL3416058 | — | — | 1 | 5.21 |
| CHEMBL3416050 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | EC50 | = | 0.92 | nM | 9.04 |
| CHEMBL3416033 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3416053 | — | EC50 | = | 422.0 | nM | 6.38 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 478.0 | nM | 6.32 |
| CHEMBL3416055 | — | EC50 | = | 632.0 | nM | 6.20 |
| CHEMBL3416060 | — | EC50 | = | 735.0 | nM | 6.13 |
| CHEMBL3416057 | — | EC50 | = | 839.0 | nM | 6.08 |
| CHEMBL3416039 | — | EC50 | = | 997.0 | nM | 6.00 |
| CHEMBL3416056 | — | EC50 | = | 1485.0 | nM | 5.83 |
| CHEMBL3416051 | — | EC50 | = | 1688.0 | nM | 5.77 |
| CHEMBL3416061 | — | EC50 | = | 1994.0 | nM | 5.70 |
| CHEMBL3416047 | — | EC50 | = | 2211.0 | nM | 5.66 |
| CHEMBL3416032 | — | EC50 | = | 2307.0 | nM | 5.64 |
| CHEMBL3416040 | — | EC50 | = | 3034.0 | nM | 5.52 |
| CHEMBL3416034 | — | EC50 | = | 3004.0 | nM | 5.52 |
| CHEMBL3416035 | — | EC50 | = | 3436.0 | nM | 5.46 |
| CHEMBL3416046 | — | EC50 | = | 4295.0 | nM | 5.37 |
| CHEMBL3416048 | — | EC50 | = | 4411.0 | nM | 5.36 |
| CHEMBL3416049 | — | EC50 | = | 4602.0 | nM | 5.34 |
| CHEMBL3416054 | — | EC50 | = | 4521.0 | nM | 5.34 |
| CHEMBL3416059 | — | EC50 | = | 4911.0 | nM | 5.31 |
| CHEMBL3416041 | — | EC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL3416042 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3416038 | — | EC50 | = | 5660.0 | nM | 5.25 |
| CHEMBL3416052 | — | EC50 | = | 6094.0 | nM | 5.21 |
| CHEMBL3416058 | — | EC50 | = | 6166.0 | nM | 5.21 |
| CHEMBL3416050 | — | EC50 | = | 6877.0 | nM | 5.16 |