Assay Detail
Binding
CHEMBL5721354
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-N-Methylspiperone from DRD2 F3.28L mutant in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay
18
Total Activities
9
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 | 18 | 6.61 | 9.24 |
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 | 9.24 |
| CHEMBL20734 | NEMONAPRIDE | 2.0 | 2 | 9.22 |
| CHEMBL81330 | — | — | 2 | 6.15 |
| CHEMBL267014 | L-745870 | — | 2 | 6.13 |
| CHEMBL444309 | — | — | 2 | 5.85 |
| CHEMBL45244 | PD-168,077 | — | 2 | 5.77 |
| CHEMBL59 | DOPAMINE | 4.0 | 2 | 5.76 |
| CHEMBL1616116 | — | — | 2 | 5.75 |
| CHEMBL103772 | — | — | 2 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267932 | MESPIPERONE | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL267932 | MESPIPERONE | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL20734 | NEMONAPRIDE | Ki | = | 0.6026 | nM | 9.22 |
| CHEMBL20734 | NEMONAPRIDE | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL81330 | — | Ki | = | 711.0 | nM | 6.15 |
| CHEMBL81330 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL267014 | L-745870 | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL267014 | L-745870 | Ki | = | 751.0 | nM | 6.12 |
| CHEMBL444309 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL444309 | — | Ki | = | 1432.0 | nM | 5.84 |
| CHEMBL45244 | PD-168,077 | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL59 | DOPAMINE | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL1616116 | — | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL103772 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL59 | DOPAMINE | Ki | = | 1829.0 | nM | 5.74 |
| CHEMBL103772 | — | Ki | = | 1866.0 | nM | 5.73 |
| CHEMBL1616116 | — | Ki | = | 1863.0 | nM | 5.73 |
| CHEMBL45244 | PD-168,077 | Ki | = | 2108.0 | nM | 5.68 |