Assay Detail
Binding
CHEMBL5235409
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Binding affinity to human D2R assessed as inhibition constant
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Recent findings leading to the discovery of selective dopamine D<sub>4</sub> receptor ligands for the treatment of widespread diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.55 | 7.39 |
| K | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.39 |
| CHEMBL81330 | — | — | 1 | 6.70 |
| CHEMBL346389 | — | — | 1 | 6.38 |
| CHEMBL5272162 | — | — | 1 | 5.68 |
| CHEMBL140099 | — | — | 1 | 5.51 |
| CHEMBL7927 | FAUC 113 | — | 1 | 5.50 |
| CHEMBL310843 | — | — | 1 | 5.47 |
| CHEMBL5278853 | — | — | 1 | 5.31 |
| CHEMBL5285358 | — | — | 1 | 5.06 |
| CHEMBL5280364 | — | — | 1 | 4.66 |
| CHEMBL143761 | — | — | 1 | 4.55 |
| CHEMBL160626 | — | — | 1 | 4.36 |
| CHEMBL66227 | — | — | 1 | - |
| CHEMBL104497 | — | — | 1 | - |
| CHEMBL1616116 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL81330 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL346389 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL5272162 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL140099 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL7927 | FAUC 113 | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL310843 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL5278853 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL5285358 | — | Ki | = | 8800.0 | nM | 5.06 |
| CHEMBL5280364 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL143761 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL160626 | — | Ki | = | 44000.0 | nM | 4.36 |
| CHEMBL66227 | — | Ki | > | 3310.0 | nM | - |
| CHEMBL104497 | — | K | > | 10000.0 | nM | - |
| CHEMBL1616116 | — | Ki | > | 1000.0 | nM | - |