Assay Detail
Binding
CHEMBL3239710
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Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis
15
Total Activities
15
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
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.27 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.70 |
| CHEMBL445102 | — | — | 1 | 7.31 |
| CHEMBL1200270 | — | — | 1 | 7.06 |
| CHEMBL3234537 | — | — | 1 | 6.89 |
| CHEMBL3234536 | — | — | 1 | 6.64 |
| CHEMBL3234543 | — | — | 1 | 6.46 |
| CHEMBL3234541 | — | — | 1 | 6.43 |
| CHEMBL3234538 | — | — | 1 | 6.06 |
| CHEMBL3234237 | JNJ-37822681 | 2.0 | 1 | 5.94 |
| CHEMBL1503220 | — | — | 1 | 5.72 |
| CHEMBL3234539 | — | — | 1 | 5.47 |
| CHEMBL3234544 | — | — | 1 | 5.39 |
| CHEMBL3234522 | — | — | 1 | 5.04 |
| CHEMBL3234542 | — | — | 1 | 4.68 |
| CHEMBL3234545 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL445102 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL1200270 | — | Ki | = | 87.6 | nM | 7.06 |
| CHEMBL3234537 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3234536 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL3234543 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL3234541 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL3234538 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL3234237 | JNJ-37822681 | Ki | = | 1159.0 | nM | 5.94 |
| CHEMBL1503220 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL3234539 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL3234544 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL3234522 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL3234542 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL3234545 | — | Ki | > | 50000.0 | nM | - |