Assay Detail
Binding
CHEMBL4825014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from human D3 receptor transfected in HEK293 cell membrane measured after 50 mins by competitive radioligand binding analysis
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.96 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854351 | — | — | 1 | 9.01 |
| CHEMBL4864112 | — | — | 1 | 8.97 |
| CHEMBL4855879 | — | — | 1 | 8.91 |
| CHEMBL25236 | BP-897 | — | 1 | 8.90 |
| CHEMBL70565 | — | — | 1 | 8.74 |
| CHEMBL4875181 | — | — | 1 | 8.28 |
| CHEMBL4852472 | — | — | 1 | 8.18 |
| CHEMBL4863032 | — | — | 1 | 8.17 |
| CHEMBL4862320 | — | — | 1 | 8.12 |
| CHEMBL4853503 | — | — | 1 | 8.07 |
| CHEMBL4862790 | — | — | 1 | 8.04 |
| CHEMBL4875008 | — | — | 1 | 7.98 |
| CHEMBL4848907 | — | — | 1 | 7.93 |
| CHEMBL4849734 | — | — | 1 | 7.89 |
| CHEMBL4860687 | — | — | 1 | 7.89 |
| CHEMBL4845838 | — | — | 1 | 7.87 |
| CHEMBL4864813 | — | — | 1 | 7.86 |
| CHEMBL4848710 | — | — | 1 | 7.86 |
| CHEMBL4878501 | — | — | 1 | 7.86 |
| CHEMBL4862399 | — | — | 1 | 7.80 |
| CHEMBL4878826 | — | — | 1 | 7.75 |
| CHEMBL4864074 | — | — | 1 | 7.74 |
| CHEMBL4855711 | — | — | 1 | 7.73 |
| CHEMBL4877715 | — | — | 1 | 7.70 |
| CHEMBL4864969 | — | — | 1 | 7.70 |
| CHEMBL4878577 | — | — | 1 | 7.63 |
| CHEMBL4853993 | — | — | 1 | 7.58 |
| CHEMBL4862275 | — | — | 1 | 7.47 |
| CHEMBL4869122 | — | — | 1 | 7.47 |
| CHEMBL4854126 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854351 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL4864112 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL4855879 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL25236 | BP-897 | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL70565 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL4875181 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4852472 | — | Ki | = | 6.58 | nM | 8.18 |
| CHEMBL4863032 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL4862320 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL4853503 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL4862790 | — | Ki | = | 9.16 | nM | 8.04 |
| CHEMBL4875008 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL4848907 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4849734 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL4860687 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL4845838 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL4878501 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL4848710 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL4864813 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL4862399 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL4878826 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL4864074 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL4855711 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL4877715 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL4864969 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL4878577 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL4853993 | — | Ki | = | 26.6 | nM | 7.58 |
| CHEMBL4862275 | — | Ki | = | 33.6 | nM | 7.47 |
| CHEMBL4869122 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL4854126 | — | Ki | = | 43.8 | nM | 7.36 |
| CHEMBL4869668 | — | Ki | = | 63.8 | nM | 7.20 |
| CHEMBL4848199 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL4875857 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4864522 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4858083 | — | Ki | > | 1000.0 | nM | - |