Assay Detail
Binding
CHEMBL3239709
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Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK 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 | 7.17 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1200270 | — | — | 1 | 9.05 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.85 |
| CHEMBL445102 | — | — | 1 | 8.12 |
| CHEMBL3234537 | — | — | 1 | 7.64 |
| CHEMBL3234536 | — | — | 1 | 7.05 |
| CHEMBL3234544 | — | — | 1 | 7.00 |
| CHEMBL3234237 | JNJ-37822681 | 2.0 | 1 | 6.80 |
| CHEMBL3234522 | — | — | 1 | 6.72 |
| CHEMBL3234543 | — | — | 1 | 6.68 |
| CHEMBL3234541 | — | — | 1 | 6.62 |
| CHEMBL3234539 | — | — | 1 | 6.54 |
| CHEMBL1503220 | — | — | 1 | 6.52 |
| CHEMBL3234542 | — | — | 1 | 6.51 |
| CHEMBL3234538 | — | — | 1 | 6.28 |
| CHEMBL3234545 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1200270 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL445102 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3234537 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3234536 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL3234544 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3234237 | JNJ-37822681 | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL3234522 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL3234543 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3234541 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3234539 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL1503220 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3234542 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL3234538 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL3234545 | — | Ki | > | 50000.0 | nM | - |