Assay Detail
Binding
CHEMBL3771916
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Displacement of [3H]-Raclopride from human dopamine D2L receptor expressed in HEK293 cells
16
Total Activities
16
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
Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.99 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.05 |
| CHEMBL3769534 | — | — | 1 | 6.90 |
| CHEMBL3771222 | — | — | 1 | 6.58 |
| CHEMBL3771309 | — | — | 1 | 6.52 |
| CHEMBL3302600 | — | — | 1 | 6.15 |
| CHEMBL3769606 | — | — | 1 | 6.08 |
| CHEMBL3770639 | — | — | 1 | 6.03 |
| CHEMBL3770473 | — | — | 1 | 5.77 |
| CHEMBL3769612 | — | — | 1 | 5.74 |
| CHEMBL3770581 | — | — | 1 | 5.70 |
| CHEMBL3770110 | — | — | 1 | 5.65 |
| CHEMBL3769836 | — | — | 1 | 5.54 |
| CHEMBL3770522 | — | — | 1 | 5.37 |
| CHEMBL3769441 | — | — | 1 | 5.29 |
| CHEMBL3770293 | — | — | 1 | 5.25 |
| CHEMBL3769536 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3769534 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL3771222 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL3771309 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL3302600 | — | Ki | = | 715.0 | nM | 6.15 |
| CHEMBL3769606 | — | Ki | = | 839.0 | nM | 6.08 |
| CHEMBL3770639 | — | Ki | = | 931.0 | nM | 6.03 |
| CHEMBL3770473 | — | Ki | = | 1709.0 | nM | 5.77 |
| CHEMBL3769612 | — | Ki | = | 1814.0 | nM | 5.74 |
| CHEMBL3770581 | — | Ki | = | 1976.0 | nM | 5.70 |
| CHEMBL3770110 | — | Ki | = | 2261.0 | nM | 5.65 |
| CHEMBL3769836 | — | Ki | = | 2906.0 | nM | 5.54 |
| CHEMBL3770522 | — | Ki | = | 4255.0 | nM | 5.37 |
| CHEMBL3769441 | — | Ki | = | 5187.0 | nM | 5.29 |
| CHEMBL3770293 | — | Ki | = | 5641.0 | nM | 5.25 |
| CHEMBL3769536 | — | Ki | = | 6790.0 | nM | 5.17 |