Assay Detail
Binding
CHEMBL672652
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Inhibition of [3H]- spiperone binding to rat brain Dopamine receptor D2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.19 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416047 | — | — | 1 | 7.92 |
| CHEMBL38969 | — | — | 1 | 7.75 |
| CHEMBL40903 | — | — | 1 | 7.64 |
| CHEMBL40082 | — | — | 1 | 7.46 |
| CHEMBL39016 | — | — | 1 | 7.37 |
| CHEMBL287760 | — | — | 1 | 7.32 |
| CHEMBL291296 | — | — | 1 | 7.12 |
| CHEMBL38473 | — | — | 1 | 7.12 |
| CHEMBL40497 | — | — | 1 | 7.09 |
| CHEMBL432284 | — | — | 1 | 6.70 |
| CHEMBL290959 | — | — | 1 | 6.41 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416047 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL38969 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL40903 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL40082 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL39016 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL287760 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL291296 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL38473 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL40497 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL432284 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL290959 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 480.0 | nM | 6.32 |