Assay Detail
Binding
CHEMBL672162
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Displacement of [3H]-YM 09151 from D2 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.79 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68191 | — | — | 1 | 7.68 |
| CHEMBL345438 | — | — | 1 | 7.58 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.95 |
| CHEMBL352207 | — | — | 1 | 6.94 |
| CHEMBL349833 | — | — | 1 | 6.86 |
| CHEMBL351989 | — | — | 1 | 6.78 |
| CHEMBL439646 | — | — | 1 | 6.70 |
| CHEMBL351963 | — | — | 1 | 6.68 |
| CHEMBL354699 | — | — | 1 | 6.66 |
| CHEMBL351612 | — | — | 1 | 6.50 |
| CHEMBL69584 | — | — | 1 | 6.16 |
| CHEMBL159742 | — | — | 1 | 6.02 |
| CHEMBL67414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68191 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL345438 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL42 | CLOZAPINE | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL352207 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL349833 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL351989 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL439646 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL351963 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL354699 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL351612 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL69584 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL159742 | — | Ki | = | 952.0 | nM | 6.02 |
| CHEMBL67414 | — | Ki | > | 1000.0 | nM | - |