Assay Detail
Binding
CHEMBL5721348
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-N-Methylspiperone from DRD4 F2.61V / L3.28F mutant in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay
23
Total Activities
14
Compounds Tested
1
Activity Types
6
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
D<sub>4</sub> dopamine receptor high-resolution structures enable the discovery of selective agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.90 | 8.60 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0005090 |
| EFO_ID | EFO_ID | - | — | MONDO:0005180 |
| EFO_ID | EFO_ID | - | — | HP:0100543 |
| EFO_TERM | EFO_TERM | - | — | schizophrenia |
| EFO_TERM | EFO_TERM | - | — | parkinson disease |
| EFO_TERM | EFO_TERM | - | — | cognitive impairment |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267932 | MESPIPERONE | 2.0 | 2 | 8.60 |
| CHEMBL20734 | NEMONAPRIDE | 2.0 | 2 | 8.21 |
| CHEMBL59 | DOPAMINE | 4.0 | 2 | 6.95 |
| CHEMBL444309 | — | — | 2 | 6.81 |
| CHEMBL81330 | — | — | 2 | 6.68 |
| CHEMBL267014 | L-745870 | — | 2 | 6.59 |
| CHEMBL103772 | — | — | 2 | 6.56 |
| CHEMBL45244 | PD-168,077 | — | 2 | 6.55 |
| CHEMBL1616116 | — | — | 2 | 5.20 |
| CHEMBL4998385 | — | — | 1 | - |
| CHEMBL5289845 | — | — | 1 | - |
| CHEMBL5722948 | — | — | 1 | - |
| CHEMBL5722985 | — | — | 1 | - |
| CHEMBL3480577 | UCSF924 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267932 | MESPIPERONE | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL267932 | MESPIPERONE | Ki | = | 2.67 | nM | 8.57 |
| CHEMBL20734 | NEMONAPRIDE | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL20734 | NEMONAPRIDE | Ki | = | 6.27 | nM | 8.20 |
| CHEMBL59 | DOPAMINE | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL59 | DOPAMINE | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL444309 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL444309 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL81330 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL81330 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL267014 | L-745870 | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL267014 | L-745870 | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL103772 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL45244 | PD-168,077 | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL45244 | PD-168,077 | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL103772 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1616116 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL1616116 | — | Ki | = | 6820.0 | nM | 5.17 |
| CHEMBL4998385 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5289845 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5722948 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5722985 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3480577 | UCSF924 | Ki | > | 10000.0 | nM | - |