Assay Detail
Binding
CHEMBL4825013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone from human D2 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 | 6.20 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70565 | — | — | 1 | 7.37 |
| CHEMBL25236 | BP-897 | — | 1 | 7.16 |
| CHEMBL4855711 | — | — | 1 | 6.38 |
| CHEMBL4878826 | — | — | 1 | 6.33 |
| CHEMBL4862399 | — | — | 1 | 6.25 |
| CHEMBL4862320 | — | — | 1 | 6.25 |
| CHEMBL4848710 | — | — | 1 | 6.25 |
| CHEMBL4864813 | — | — | 1 | 6.23 |
| CHEMBL4864969 | — | — | 1 | 6.19 |
| CHEMBL4878577 | — | — | 1 | 6.18 |
| CHEMBL4862275 | — | — | 1 | 6.16 |
| CHEMBL4864112 | — | — | 1 | 6.16 |
| CHEMBL4863032 | — | — | 1 | 6.15 |
| CHEMBL4878501 | — | — | 1 | 6.14 |
| CHEMBL4869668 | — | — | 1 | 6.14 |
| CHEMBL4862790 | — | — | 1 | 6.13 |
| CHEMBL4854351 | — | — | 1 | 6.13 |
| CHEMBL4875008 | — | — | 1 | 6.11 |
| CHEMBL4853993 | — | — | 1 | 6.11 |
| CHEMBL4848199 | — | — | 1 | 6.11 |
| CHEMBL4852472 | — | — | 1 | 6.09 |
| CHEMBL4848907 | — | — | 1 | 6.07 |
| CHEMBL4877715 | — | — | 1 | 6.07 |
| CHEMBL4849734 | — | — | 1 | 6.06 |
| CHEMBL4845838 | — | — | 1 | 6.05 |
| CHEMBL4875181 | — | — | 1 | 6.04 |
| CHEMBL4855879 | — | — | 1 | 6.02 |
| CHEMBL4869122 | — | — | 1 | 6.02 |
| CHEMBL4853503 | — | — | 1 | 6.02 |
| CHEMBL4860687 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70565 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL25236 | BP-897 | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4855711 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL4878826 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL4862399 | — | Ki | = | 563.0 | nM | 6.25 |
| CHEMBL4862320 | — | Ki | = | 568.0 | nM | 6.25 |
| CHEMBL4848710 | — | Ki | = | 568.0 | nM | 6.25 |
| CHEMBL4864813 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL4864969 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL4878577 | — | Ki | = | 663.0 | nM | 6.18 |
| CHEMBL4862275 | — | Ki | = | 688.0 | nM | 6.16 |
| CHEMBL4864112 | — | Ki | = | 697.0 | nM | 6.16 |
| CHEMBL4863032 | — | Ki | = | 708.0 | nM | 6.15 |
| CHEMBL4878501 | — | Ki | = | 723.0 | nM | 6.14 |
| CHEMBL4869668 | — | Ki | = | 728.0 | nM | 6.14 |
| CHEMBL4862790 | — | Ki | = | 744.0 | nM | 6.13 |
| CHEMBL4854351 | — | Ki | = | 732.0 | nM | 6.13 |
| CHEMBL4875008 | — | Ki | = | 785.0 | nM | 6.11 |
| CHEMBL4848199 | — | Ki | = | 776.0 | nM | 6.11 |
| CHEMBL4853993 | — | Ki | = | 785.0 | nM | 6.11 |
| CHEMBL4852472 | — | Ki | = | 803.0 | nM | 6.09 |
| CHEMBL4848907 | — | Ki | = | 853.0 | nM | 6.07 |
| CHEMBL4877715 | — | Ki | = | 861.0 | nM | 6.07 |
| CHEMBL4849734 | — | Ki | = | 863.0 | nM | 6.06 |
| CHEMBL4845838 | — | Ki | = | 897.0 | nM | 6.05 |
| CHEMBL4875181 | — | Ki | = | 923.0 | nM | 6.04 |
| CHEMBL4855879 | — | Ki | = | 962.0 | nM | 6.02 |
| CHEMBL4869122 | — | Ki | = | 962.0 | nM | 6.02 |
| CHEMBL4853503 | — | Ki | = | 958.0 | nM | 6.02 |
| CHEMBL4860687 | — | Ki | = | 967.0 | nM | 6.01 |
| CHEMBL4854126 | — | Ki | = | 1025.0 | nM | 5.99 |
| CHEMBL4864074 | — | Ki | = | 1065.0 | nM | 5.97 |
| CHEMBL4875857 | — | Ki | - | — | - | |
| CHEMBL4864522 | — | Ki | - | — | - | |
| CHEMBL4858083 | — | Ki | - | — | - |