Assay Detail
Binding
CHEMBL674499
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Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.27 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267014 | L-745870 | — | 1 | 9.04 |
| CHEMBL149596 | — | — | 1 | 8.74 |
| CHEMBL151286 | — | — | 1 | 8.59 |
| CHEMBL147059 | — | — | 1 | 8.59 |
| CHEMBL346398 | — | — | 1 | 8.55 |
| CHEMBL146757 | — | — | 1 | 8.42 |
| CHEMBL346389 | — | — | 1 | 8.37 |
| CHEMBL345552 | — | — | 1 | 8.37 |
| CHEMBL150129 | — | — | 1 | 8.30 |
| CHEMBL150181 | — | — | 1 | 8.29 |
| CHEMBL149233 | — | — | 1 | 8.21 |
| CHEMBL149497 | — | — | 1 | 8.17 |
| CHEMBL151533 | — | — | 1 | 8.16 |
| CHEMBL150173 | — | — | 1 | 7.97 |
| CHEMBL348435 | — | — | 1 | 7.91 |
| CHEMBL147130 | — | — | 1 | 7.74 |
| CHEMBL147011 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267014 | L-745870 | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL149596 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL151286 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL147059 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL346398 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL146757 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL346389 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL345552 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL150129 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL150181 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL149233 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL149497 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL151533 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL150173 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL348435 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL147130 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL147011 | — | Ki | = | 62.4 | nM | 7.21 |