Assay Detail
Binding
CHEMBL4314365
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.96 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 9.52 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 9.47 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 9.31 |
| CHEMBL1237021 | LURASIDONE | 4.0 | 1 | 8.77 |
| CHEMBL2377590 | — | — | 1 | 7.85 |
| CHEMBL4483554 | — | — | 1 | 7.80 |
| CHEMBL4515160 | — | — | 1 | 7.72 |
| CHEMBL4454176 | — | — | 1 | 7.70 |
| CHEMBL4571321 | — | — | 1 | 7.21 |
| CHEMBL2377591 | — | — | 1 | 6.79 |
| CHEMBL4571862 | — | — | 1 | 6.72 |
| CHEMBL4591440 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL1237021 | LURASIDONE | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2377590 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4483554 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4515160 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4454176 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4571321 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL2377591 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4571862 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL4591440 | — | Ki | = | 217.0 | nM | 6.66 |