Assay Detail
Functional
CHEMBL3419954
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Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
36
Total Activities
36
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 | 36 | 6.84 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 9.68 |
| CHEMBL3416067 | — | — | 1 | 8.47 |
| CHEMBL360328 | LORCASERIN | 4.0 | 1 | 8.44 |
| CHEMBL3416063 | — | — | 1 | 8.38 |
| CHEMBL3416061 | — | — | 1 | 7.96 |
| CHEMBL3416033 | — | — | 1 | 7.89 |
| CHEMBL3416065 | — | — | 1 | 7.66 |
| CHEMBL3416055 | — | — | 1 | 7.50 |
| CHEMBL3416047 | — | — | 1 | 7.22 |
| CHEMBL3416049 | — | — | 1 | 7.20 |
| CHEMBL3416039 | — | — | 1 | 7.04 |
| CHEMBL3416057 | — | — | 1 | 7.04 |
| CHEMBL3416035 | — | — | 1 | 6.99 |
| CHEMBL3416051 | — | — | 1 | 6.88 |
| CHEMBL3416062 | — | — | 1 | 6.80 |
| CHEMBL3416043 | — | — | 1 | 6.74 |
| CHEMBL3416059 | — | — | 1 | 6.69 |
| CHEMBL3416053 | — | — | 1 | 6.67 |
| CHEMBL3416045 | — | — | 1 | 6.61 |
| CHEMBL3416041 | — | — | 1 | 6.60 |
| CHEMBL3416037 | — | — | 1 | 6.54 |
| CHEMBL3416060 | — | — | 1 | 6.53 |
| CHEMBL3416048 | — | — | 1 | 6.44 |
| CHEMBL3416066 | — | — | 1 | 6.29 |
| CHEMBL3416032 | — | — | 1 | 6.19 |
| CHEMBL3416042 | — | — | 1 | 6.18 |
| CHEMBL3416036 | — | — | 1 | 6.17 |
| CHEMBL3416046 | — | — | 1 | 6.13 |
| CHEMBL3416056 | — | — | 1 | 6.04 |
| CHEMBL3416064 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL3416067 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3416063 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3416061 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3416033 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3416065 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3416055 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3416047 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3416049 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3416039 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3416057 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3416035 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL3416051 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL3416062 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL3416043 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3416059 | — | EC50 | = | 206.0 | nM | 6.69 |
| CHEMBL3416053 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL3416045 | — | EC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3416041 | — | EC50 | = | 251.0 | nM | 6.60 |
| CHEMBL3416037 | — | EC50 | = | 288.0 | nM | 6.54 |
| CHEMBL3416060 | — | EC50 | = | 296.0 | nM | 6.53 |
| CHEMBL3416048 | — | EC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3416066 | — | EC50 | = | 514.0 | nM | 6.29 |
| CHEMBL3416032 | — | EC50 | = | 646.0 | nM | 6.19 |
| CHEMBL3416042 | — | EC50 | = | 667.0 | nM | 6.18 |
| CHEMBL3416036 | — | EC50 | = | 683.0 | nM | 6.17 |
| CHEMBL3416046 | — | EC50 | = | 737.0 | nM | 6.13 |
| CHEMBL3416056 | — | EC50 | = | 914.0 | nM | 6.04 |
| CHEMBL3416064 | — | EC50 | = | 985.0 | nM | 6.01 |
| CHEMBL3416040 | — | EC50 | = | 1082.0 | nM | 5.97 |
| CHEMBL3416054 | — | EC50 | = | 1127.0 | nM | 5.95 |
| CHEMBL3416034 | — | EC50 | = | 1228.0 | nM | 5.91 |
| CHEMBL3416058 | — | EC50 | = | 1258.0 | nM | 5.90 |
| CHEMBL3416044 | — | EC50 | = | 1762.0 | nM | 5.75 |
| CHEMBL3416038 | — | EC50 | = | 2481.0 | nM | 5.61 |