Assay Detail
Binding
CHEMBL677318
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Inhibition of enkephalinase activity in synaptic membranes prepared from rat striatum
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.49 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL479579 | PHOSPHORAMIDON | — | 1 | 9.22 |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.52 |
| CHEMBL85397 | — | — | 1 | 8.40 |
| CHEMBL83778 | — | — | 1 | 8.40 |
| CHEMBL85159 | — | — | 1 | 8.30 |
| CHEMBL85560 | — | — | 1 | 8.22 |
| CHEMBL295104 | — | — | 1 | 8.10 |
| CHEMBL314855 | — | — | 1 | 8.05 |
| CHEMBL83326 | — | — | 1 | 7.92 |
| CHEMBL47289 | — | — | 1 | 7.75 |
| CHEMBL430436 | — | — | 1 | 7.70 |
| CHEMBL315312 | — | — | 1 | 7.60 |
| CHEMBL311093 | — | — | 1 | 7.54 |
| CHEMBL82732 | — | — | 1 | 7.42 |
| CHEMBL84930 | — | — | 1 | 7.40 |
| CHEMBL421724 | — | — | 1 | 7.13 |
| CHEMBL85324 | — | — | 1 | 7.05 |
| CHEMBL84195 | — | — | 1 | 6.10 |
| CHEMBL313766 | — | — | 1 | 6.00 |
| CHEMBL84865 | — | — | 1 | 6.00 |
| CHEMBL84370 | — | — | 1 | 6.00 |
| CHEMBL84258 | — | — | 1 | 6.00 |
| CHEMBL86222 | — | — | 1 | - |
| CHEMBL84924 | — | — | 1 | - |
| CHEMBL2114199 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL479579 | PHOSPHORAMIDON | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL10247 | THIORPHAN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL85397 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL83778 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL85159 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL85560 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL295104 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL314855 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL83326 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL47289 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL430436 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL315312 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL311093 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL82732 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL84930 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL421724 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL85324 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL84195 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL313766 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL84865 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL84370 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL84258 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL86222 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL84924 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2114199 | — | IC50 | > | 1000.0 | nM | - |