Assay Detail
Binding
CHEMBL4314362
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 31 | 7.54 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 9.92 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.77 |
| CHEMBL4591440 | — | — | 1 | 8.64 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 1 | 8.59 |
| CHEMBL4454176 | — | — | 1 | 8.49 |
| CHEMBL4571321 | — | — | 1 | 8.31 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.26 |
| CHEMBL4483554 | — | — | 1 | 8.20 |
| CHEMBL1237021 | LURASIDONE | 4.0 | 1 | 8.17 |
| CHEMBL4515160 | — | — | 1 | 8.15 |
| CHEMBL439849 | VILAZODONE | 4.0 | 1 | 8.01 |
| CHEMBL4571862 | — | — | 1 | 7.89 |
| CHEMBL1200938 | METHYSERGIDE MALEATE | 4.0 | 1 | 7.77 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.68 |
| CHEMBL4567029 | — | — | 1 | 7.31 |
| CHEMBL4437024 | — | — | 1 | 7.28 |
| CHEMBL4451635 | — | — | 1 | 7.16 |
| CHEMBL4567158 | — | — | 1 | 7.11 |
| CHEMBL4474439 | — | — | 1 | 6.91 |
| CHEMBL4470604 | — | — | 1 | 6.84 |
| CHEMBL4587314 | — | — | 1 | 6.80 |
| CHEMBL4461080 | — | — | 1 | 6.74 |
| CHEMBL4482920 | — | — | 1 | 6.69 |
| CHEMBL4461198 | — | — | 1 | 6.65 |
| CHEMBL4456442 | — | — | 1 | 6.62 |
| CHEMBL4553259 | — | — | 1 | 6.61 |
| CHEMBL4591262 | — | — | 1 | 6.50 |
| CHEMBL4470395 | — | — | 1 | 6.47 |
| CHEMBL4472066 | — | — | 1 | 6.16 |
| CHEMBL4572132 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4591440 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2028019 | CARIPRAZINE | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4454176 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4571321 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL39 | SEROTONIN | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4483554 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL1237021 | LURASIDONE | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL4515160 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL439849 | VILAZODONE | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL4571862 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1200938 | METHYSERGIDE MALEATE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL49 | BUSPIRONE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4567029 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL4437024 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4451635 | — | Ki | = | 68.7 | nM | 7.16 |
| CHEMBL4567158 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4474439 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL4470604 | — | Ki | = | 143.2 | nM | 6.84 |
| CHEMBL4587314 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4461080 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4482920 | — | Ki | = | 204.1 | nM | 6.69 |
| CHEMBL4461198 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL4456442 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4553259 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL4591262 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL4470395 | — | Ki | = | 336.0 | nM | 6.47 |
| CHEMBL4472066 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL4572132 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL11 | IMIPRAMINE | Ki | - | — | - |