Assay Detail
ADMET
CHEMBL4013758
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Agonist activity at human 5-HT2B receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
28
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 6.88 | 8.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | 3.0 | 2 | 8.84 |
| CHEMBL4091672 | — | — | 2 | 7.62 |
| CHEMBL4086286 | — | — | 2 | 7.25 |
| CHEMBL4064935 | — | — | 2 | 7.06 |
| CHEMBL4082227 | — | — | 2 | 7.05 |
| CHEMBL4075150 | — | — | 2 | 7.02 |
| CHEMBL4063893 | — | — | 2 | 6.95 |
| CHEMBL4064809 | — | — | 2 | 6.62 |
| CHEMBL4094164 | — | — | 2 | 6.56 |
| CHEMBL4094054 | — | — | 2 | 6.48 |
| CHEMBL360328 | LORCASERIN | 4.0 | 2 | 6.36 |
| CHEMBL4101194 | — | — | 2 | 6.24 |
| CHEMBL4090984 | — | — | 2 | 6.19 |
| CHEMBL4073529 | — | — | 2 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39 | SEROTONIN | EC50 | = | 1.445 | nM | 8.84 |
| CHEMBL39 | SEROTONIN | EC50 | = | 1.46 | nM | 8.84 |
| CHEMBL4091672 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4091672 | — | EC50 | = | 24.55 | nM | 7.61 |
| CHEMBL4086286 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4086286 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4064935 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4064935 | — | EC50 | = | 87.1 | nM | 7.06 |
| CHEMBL4082227 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4082227 | — | EC50 | = | 89.13 | nM | 7.05 |
| CHEMBL4075150 | — | EC50 | = | 95.5 | nM | 7.02 |
| CHEMBL4075150 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4063893 | — | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL4063893 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4064809 | — | EC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4064809 | — | EC50 | = | 239.88 | nM | 6.62 |
| CHEMBL4094164 | — | EC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4094164 | — | EC50 | = | 275.42 | nM | 6.56 |
| CHEMBL4094054 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL4094054 | — | EC50 | = | 335.0 | nM | 6.47 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 433.0 | nM | 6.36 |
| CHEMBL360328 | LORCASERIN | EC50 | = | 436.52 | nM | 6.36 |
| CHEMBL4101194 | — | EC50 | = | 575.44 | nM | 6.24 |
| CHEMBL4101194 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4090984 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL4090984 | — | EC50 | = | 641.0 | nM | 6.19 |
| CHEMBL4073529 | — | EC50 | = | 812.83 | nM | 6.09 |
| CHEMBL4073529 | — | EC50 | = | 807.0 | nM | 6.09 |