Assay Detail
Binding
CHEMBL4048885
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 19 | 8.12 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096543 | — | — | 1 | 9.48 |
| CHEMBL3354065 | — | — | 1 | 9.01 |
| CHEMBL4072818 | — | — | 1 | 8.90 |
| CHEMBL4080675 | — | — | 1 | 8.86 |
| CHEMBL4091231 | — | — | 1 | 8.71 |
| CHEMBL320597 | — | — | 1 | 8.70 |
| CHEMBL4093527 | — | — | 1 | 8.67 |
| CHEMBL267014 | L-745870 | — | 1 | 8.65 |
| CHEMBL4080034 | — | — | 1 | 8.55 |
| CHEMBL4085780 | — | — | 1 | 8.54 |
| CHEMBL3354073 | — | — | 1 | 8.36 |
| CHEMBL4098720 | — | — | 1 | 8.28 |
| CHEMBL4091058 | — | — | 1 | 7.70 |
| CHEMBL4063176 | — | — | 1 | 7.54 |
| CHEMBL3354072 | — | — | 1 | 7.13 |
| CHEMBL4079495 | — | — | 1 | 7.02 |
| CHEMBL3354074 | — | — | 1 | 7.00 |
| CHEMBL4074104 | — | — | 1 | 6.59 |
| CHEMBL4064222 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096543 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL3354065 | — | Ki | = | 0.9772 | nM | 9.01 |
| CHEMBL4072818 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL4080675 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL4091231 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL320597 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4093527 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL267014 | L-745870 | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL4080034 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL4085780 | — | Ki | = | 2.884 | nM | 8.54 |
| CHEMBL3354073 | — | Ki | = | 4.365 | nM | 8.36 |
| CHEMBL4098720 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL4091058 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL4063176 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL3354072 | — | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL4079495 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL3354074 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4074104 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL4064222 | — | Ki | = | 316.23 | nM | 6.50 |