Assay Detail
Binding
CHEMBL672376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Corpus striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.95 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.35 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.72 |
| CHEMBL64875 | — | — | 1 | 8.18 |
| CHEMBL330603 | — | — | 1 | 7.80 |
| CHEMBL97184 | — | — | 1 | 7.70 |
| CHEMBL328048 | — | — | 1 | 7.54 |
| CHEMBL318249 | — | — | 1 | 7.37 |
| CHEMBL98299 | — | — | 1 | 7.22 |
| CHEMBL97422 | — | — | 1 | 7.10 |
| CHEMBL330171 | — | — | 1 | 7.07 |
| CHEMBL328940 | — | — | 1 | 7.07 |
| CHEMBL97650 | — | — | 1 | 7.04 |
| CHEMBL94612 | — | — | 1 | 6.85 |
| CHEMBL95169 | — | — | 1 | 6.85 |
| CHEMBL319352 | — | — | 1 | 6.85 |
| CHEMBL97242 | — | — | 1 | 6.72 |
| CHEMBL318735 | — | — | 1 | 6.70 |
| CHEMBL421573 | — | — | 1 | 6.64 |
| CHEMBL328187 | — | — | 1 | 6.51 |
| CHEMBL318901 | — | — | 1 | 6.43 |
| CHEMBL95175 | — | — | 1 | 6.40 |
| CHEMBL327662 | — | — | 1 | 6.37 |
| CHEMBL317333 | — | — | 1 | 6.31 |
| CHEMBL93923 | — | — | 1 | 6.31 |
| CHEMBL97333 | — | — | 1 | 6.27 |
| CHEMBL329280 | — | — | 1 | 6.24 |
| CHEMBL327527 | — | — | 1 | 6.18 |
| CHEMBL98241 | — | — | 1 | 6.01 |
| CHEMBL313424 | — | — | 1 | 5.64 |
| CHEMBL420997 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL64875 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL330603 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL97184 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL328048 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL318249 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL98299 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL97422 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL330171 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL328940 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL97650 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL94612 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL95169 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL319352 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL97242 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL318735 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL421573 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL328187 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL318901 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL95175 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL327662 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL317333 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL93923 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL97333 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL329280 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL327527 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL98241 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL313424 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL420997 | — | Ki | > | 2900.0 | nM | - |