Assay Detail
Binding
CHEMBL666964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.14 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.52 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 7.10 |
| CHEMBL171698 | — | — | 1 | 6.82 |
| CHEMBL435263 | — | — | 1 | 6.75 |
| CHEMBL434921 | — | — | 1 | 6.66 |
| CHEMBL170356 | — | — | 1 | 6.50 |
| CHEMBL171117 | — | — | 1 | 6.50 |
| CHEMBL368321 | — | — | 1 | 6.37 |
| CHEMBL173042 | — | — | 1 | 6.35 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.35 |
| CHEMBL354362 | — | — | 1 | 6.26 |
| CHEMBL353848 | — | — | 1 | 6.13 |
| CHEMBL170596 | — | — | 1 | 6.12 |
| CHEMBL424948 | — | — | 1 | 6.12 |
| CHEMBL449081 | AGROCLAVINE | — | 1 | 6.05 |
| CHEMBL171069 | — | — | 1 | 6.04 |
| CHEMBL172996 | — | — | 1 | 5.87 |
| CHEMBL352753 | — | — | 1 | 5.77 |
| CHEMBL171915 | — | — | 1 | 5.70 |
| CHEMBL171564 | — | — | 1 | 5.68 |
| CHEMBL171303 | — | — | 1 | 5.52 |
| CHEMBL355798 | — | — | 1 | 5.47 |
| CHEMBL366850 | — | — | 1 | 5.46 |
| CHEMBL13866 | — | — | 1 | 5.38 |
| CHEMBL353690 | — | — | 1 | 5.10 |
| CHEMBL173166 | — | — | 1 | - |
| CHEMBL368777 | — | — | 1 | - |
| CHEMBL172778 | — | — | 1 | - |
| CHEMBL174410 | — | — | 1 | - |
| CHEMBL353664 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL171698 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL435263 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL434921 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL170356 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL171117 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL368321 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL173042 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL354362 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL353848 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL170596 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL424948 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL449081 | AGROCLAVINE | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL171069 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL172996 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL352753 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL171915 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL171564 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL171303 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL355798 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL366850 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL13866 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL353690 | — | IC50 | = | 7940.0 | nM | 5.10 |
| CHEMBL173166 | — | IC50 | - | nM | - | |
| CHEMBL368777 | — | IC50 | - | nM | - | |
| CHEMBL172778 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL174410 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL353664 | — | IC50 | - | nM | - |