Assay Detail
Binding
CHEMBL3372352
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Displacement of [3H]DTG from rat liver sigma2 receptor by scintillation counting analysis in presence of pentazocine
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.88 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354886 | — | — | 1 | 10.40 |
| CHEMBL3354882 | — | — | 1 | 8.27 |
| CHEMBL583580 | — | — | 1 | 7.73 |
| CHEMBL3354876 | — | — | 1 | 7.65 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.45 |
| CHEMBL3354874 | — | — | 1 | 7.39 |
| CHEMBL3354885 | — | — | 1 | 5.79 |
| CHEMBL3354881 | — | — | 1 | 5.75 |
| CHEMBL3354879 | — | — | 1 | 5.75 |
| CHEMBL3354880 | — | — | 1 | 5.71 |
| CHEMBL3354875 | — | — | 1 | 5.49 |
| CHEMBL3354877 | — | — | 1 | 5.19 |
| CHEMBL3354878 | — | — | 1 | - |
| CHEMBL3354883 | — | — | 1 | - |
| CHEMBL3354884 | — | — | 1 | - |
| CHEMBL3352842 | — | — | 1 | - |
| CHEMBL3354887 | — | — | 1 | - |
| CHEMBL3354888 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354886 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3354882 | — | Ki | = | 5.34 | nM | 8.27 |
| CHEMBL583580 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL3354876 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 35.4 | nM | 7.45 |
| CHEMBL3354874 | — | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL3354885 | — | Ki | = | 1623.0 | nM | 5.79 |
| CHEMBL3354881 | — | Ki | = | 1761.0 | nM | 5.75 |
| CHEMBL3354879 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL3354880 | — | Ki | = | 1946.0 | nM | 5.71 |
| CHEMBL3354875 | — | Ki | = | 3210.0 | nM | 5.49 |
| CHEMBL3354877 | — | Ki | = | 6517.0 | nM | 5.19 |
| CHEMBL3354878 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354883 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354884 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3352842 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354887 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3354888 | — | Ki | > | 10000.0 | nM | - |