Assay Detail
Functional
CHEMBL3871849
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at unedited 5-HT2C receptor (unknown origin) expressed in HEK293 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by scintillation counting
43
Total Activities
42
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
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 43 | 7.72 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3947276 | — | — | 1 | 9.70 |
| CHEMBL3979806 | — | — | 1 | 9.50 |
| CHEMBL3967107 | — | — | 1 | 9.10 |
| CHEMBL3959570 | — | — | 1 | 9.10 |
| CHEMBL3956394 | — | — | 1 | 9.00 |
| CHEMBL3919795 | — | — | 1 | 8.80 |
| CHEMBL3930174 | — | — | 1 | 8.70 |
| CHEMBL3946277 | — | — | 1 | 8.60 |
| CHEMBL3912721 | — | — | 1 | 8.50 |
| CHEMBL3982618 | — | — | 1 | 8.50 |
| CHEMBL3955996 | — | — | 1 | 8.50 |
| CHEMBL3895184 | — | — | 1 | 8.40 |
| CHEMBL3928388 | — | — | 1 | 8.20 |
| CHEMBL3935339 | — | — | 1 | 8.20 |
| CHEMBL3943620 | — | — | 1 | 8.00 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | 2.0 | 1 | 7.90 |
| CHEMBL3907399 | — | — | 1 | 7.70 |
| CHEMBL3961589 | — | — | 1 | 7.70 |
| CHEMBL3978882 | — | — | 1 | 7.70 |
| CHEMBL3950846 | — | — | 1 | 7.70 |
| CHEMBL3933563 | — | — | 1 | 7.60 |
| CHEMBL3961026 | — | — | 1 | 7.60 |
| CHEMBL3938893 | — | — | 1 | 7.50 |
| CHEMBL3924644 | — | — | 1 | 7.40 |
| CHEMBL3937394 | — | — | 1 | 7.20 |
| CHEMBL3890492 | — | — | 1 | 7.20 |
| CHEMBL3919861 | — | — | 1 | 7.20 |
| CHEMBL3966227 | — | — | 1 | 7.10 |
| CHEMBL3956136 | — | — | 1 | 7.00 |
| CHEMBL3891704 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3947276 | — | EC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL3979806 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3959570 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3967107 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3956394 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3919795 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL3930174 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL3946277 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL3912721 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL3982618 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL3955996 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL3895184 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3928388 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3935339 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3943620 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL478 | CHLOROPHENYLPIPERAZINE | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3907399 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3961589 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3978882 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3950846 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3961026 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3933563 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3938893 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3924644 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3937394 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3890492 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3919861 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3966227 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3956136 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3891704 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3891802 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3899449 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3891802 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3934644 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3928762 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3975593 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3952329 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3947432 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3973690 | — | EC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3931859 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3967240 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL3895972 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3900787 | — | EC50 | > | 10000.0 | nM | - |