Assay Detail
ADMET
CHEMBL4048883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.91 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093527 | — | — | 1 | 6.54 |
| CHEMBL4091231 | — | — | 1 | 6.34 |
| CHEMBL4080675 | — | — | 1 | 6.28 |
| CHEMBL3354072 | — | — | 1 | 6.18 |
| CHEMBL3354065 | — | — | 1 | 6.17 |
| CHEMBL4098720 | — | — | 1 | 6.04 |
| CHEMBL4072818 | — | — | 1 | 6.04 |
| CHEMBL3354074 | — | — | 1 | 6.03 |
| CHEMBL4085780 | — | — | 1 | 5.96 |
| CHEMBL3354073 | — | — | 1 | 5.93 |
| CHEMBL267014 | L-745870 | — | 1 | 5.79 |
| CHEMBL4091058 | — | — | 1 | 5.42 |
| CHEMBL4074104 | — | — | 1 | 5.35 |
| CHEMBL4064222 | — | — | 1 | 5.29 |
| CHEMBL4063176 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093527 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL4091231 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL4080675 | — | Ki | = | 524.81 | nM | 6.28 |
| CHEMBL3354072 | — | Ki | = | 660.69 | nM | 6.18 |
| CHEMBL3354065 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL4098720 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL4072818 | — | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL3354074 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL4085780 | — | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL3354073 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL267014 | L-745870 | Ki | = | 1621.81 | nM | 5.79 |
| CHEMBL4091058 | — | Ki | = | 3801.89 | nM | 5.42 |
| CHEMBL4074104 | — | Ki | = | 4466.84 | nM | 5.35 |
| CHEMBL4064222 | — | Ki | = | 5128.61 | nM | 5.29 |
| CHEMBL4063176 | — | Ki | = | 5754.4 | nM | 5.24 |