Assay Detail
Functional
CHEMBL2342830
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Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
12
Total Activities
6
Compounds Tested
2
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
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.66 | 6.26 |
| Imax | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 6.26 |
| CHEMBL1457510 | — | — | 2 | 6.00 |
| CHEMBL448891 | — | — | 2 | 4.73 |
| CHEMBL286080 | SKF-38393 | — | 2 | - |
| CHEMBL39 | SEROTONIN | 3.0 | 2 | - |
| CHEMBL13668 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1457510 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL448891 | — | IC50 | = | 18730.0 | nM | 4.73 |
| CHEMBL1457510 | — | Imax | = | 58.9 | % | - |
| CHEMBL448891 | — | Imax | = | 82.3 | % | - |
| CHEMBL54 | HALOPERIDOL | Imax | = | 94.6 | % | - |
| CHEMBL286080 | SKF-38393 | Imax | - | — | - | |
| CHEMBL39 | SEROTONIN | Imax | - | — | - | |
| CHEMBL13668 | — | Imax | - | — | - | |
| CHEMBL286080 | SKF-38393 | IC50 | - | — | - | |
| CHEMBL39 | SEROTONIN | IC50 | - | — | - | |
| CHEMBL13668 | — | IC50 | - | — | - |