Assay Detail
Binding
CHEMBL675960
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Affinity was evaluated by inhibition of [3H]spiperone binding to COS cells transfected with human dopamine D-2(long) 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 | 7.27 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7617 | — | — | 1 | 9.00 |
| CHEMBL90882 | — | — | 1 | 8.60 |
| CHEMBL88464 | — | — | 1 | 8.06 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 7.68 |
| CHEMBL89970 | — | — | 1 | 7.68 |
| CHEMBL91310 | — | — | 1 | 7.24 |
| CHEMBL432762 | — | — | 1 | 7.03 |
| CHEMBL7828 | ISOLOXAPINE | — | 1 | 6.82 |
| CHEMBL88870 | — | — | 1 | 6.54 |
| CHEMBL275696 | — | — | 1 | 6.28 |
| CHEMBL328246 | — | — | 1 | 6.16 |
| CHEMBL90977 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7617 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL90882 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL88464 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL831 | LOXAPINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL89970 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL91310 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL432762 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL7828 | ISOLOXAPINE | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL88870 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL275696 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL328246 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL90977 | — | Ki | = | 730.0 | nM | 6.14 |