Assay Detail
Binding
CHEMBL673252
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Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.57 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90882 | — | — | 1 | 9.27 |
| CHEMBL88464 | — | — | 1 | 9.05 |
| CHEMBL7617 | — | — | 1 | 9.00 |
| CHEMBL89970 | — | — | 1 | 8.70 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 8.31 |
| CHEMBL432762 | — | — | 1 | 7.92 |
| CHEMBL7828 | ISOLOXAPINE | — | 1 | 7.64 |
| CHEMBL91310 | — | — | 1 | 7.33 |
| CHEMBL90977 | — | — | 1 | 6.52 |
| CHEMBL328246 | — | — | 1 | 6.03 |
| CHEMBL88870 | — | — | 1 | 5.57 |
| CHEMBL275696 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90882 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL88464 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL7617 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL89970 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL831 | LOXAPINE | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL432762 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL7828 | ISOLOXAPINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL91310 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL90977 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL328246 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL88870 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL275696 | — | Ki | = | 2900.0 | nM | 5.54 |