Assay Detail
Binding
CHEMBL679938
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In vitro binding affinity against cloned mammalian dopamine D2 autoreceptor, expressed in CHO-K1 cells, using [3H]U-86170 as radioligand
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 6.81 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7549 | PRECLAMOL | 2.0 | 1 | 8.07 |
| CHEMBL93570 | — | — | 1 | 7.96 |
| CHEMBL280955 | — | — | 1 | 7.75 |
| CHEMBL93646 | — | — | 1 | 7.66 |
| CHEMBL94811 | — | — | 1 | 7.54 |
| CHEMBL24222 | — | — | 1 | 7.30 |
| CHEMBL93917 | — | — | 1 | 7.16 |
| CHEMBL93383 | — | — | 1 | 6.97 |
| CHEMBL92183 | — | — | 1 | 6.92 |
| CHEMBL314536 | — | — | 1 | 6.87 |
| CHEMBL413483 | — | — | 1 | 6.73 |
| CHEMBL93594 | — | — | 1 | 6.72 |
| CHEMBL329443 | — | — | 1 | 6.64 |
| CHEMBL90798 | — | — | 1 | 6.63 |
| CHEMBL93101 | — | — | 1 | 6.62 |
| CHEMBL93212 | — | — | 1 | 6.59 |
| CHEMBL93682 | — | — | 1 | 6.50 |
| CHEMBL311730 | — | — | 1 | 6.35 |
| CHEMBL328894 | — | — | 1 | 6.29 |
| CHEMBL93582 | — | — | 1 | 6.22 |
| CHEMBL93946 | — | — | 1 | 6.09 |
| CHEMBL92939 | — | — | 1 | 6.01 |
| CHEMBL90662 | — | — | 1 | 5.98 |
| CHEMBL91228 | — | — | 1 | 5.93 |
| CHEMBL93900 | — | — | 1 | - |
| CHEMBL96726 | — | — | 1 | - |
| CHEMBL92232 | — | — | 1 | - |
| CHEMBL90797 | — | — | 1 | - |
| CHEMBL566970 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7549 | PRECLAMOL | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL93570 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL280955 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL93646 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL94811 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL24222 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL93917 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL93383 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL92183 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL314536 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL413483 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL93594 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL329443 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL90798 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL93101 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL93212 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL93682 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL311730 | — | Ki | = | 447.0 | nM | 6.35 |
| CHEMBL328894 | — | Ki | = | 519.0 | nM | 6.29 |
| CHEMBL93582 | — | Ki | = | 602.0 | nM | 6.22 |
| CHEMBL93946 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL92939 | — | Ki | = | 984.0 | nM | 6.01 |
| CHEMBL90662 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL91228 | — | Ki | = | 1178.0 | nM | 5.93 |
| CHEMBL93900 | — | Ki | > | 1852.0 | nM | - |
| CHEMBL96726 | — | Ki | > | 1500.0 | nM | - |
| CHEMBL92232 | — | Ki | > | 1852.0 | nM | - |
| CHEMBL90797 | — | Ki | > | 1852.0 | nM | - |
| CHEMBL566970 | — | Ki | > | 339.0 | nM | - |