Assay Detail
Binding
CHEMBL2215099
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Displacement of [3H](+)-pentazocine from rat brain sigma1 receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A σ(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.03 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL408867 | [11C]SA4503 | — | 1 | 8.33 |
| CHEMBL2205822 | — | — | 1 | 8.26 |
| CHEMBL2205831 | — | — | 1 | 8.17 |
| CHEMBL2205821 | — | — | 1 | 8.00 |
| CHEMBL2205812 | — | — | 1 | 7.82 |
| CHEMBL2205813 | — | — | 1 | 7.82 |
| CHEMBL2205820 | — | — | 1 | 7.82 |
| CHEMBL2205819 | — | — | 1 | 7.77 |
| CHEMBL2205815 | — | — | 1 | 7.58 |
| CHEMBL2205835 | — | — | 1 | 7.58 |
| CHEMBL2205811 | — | — | 1 | 7.28 |
| CHEMBL2205826 | — | — | 1 | 7.18 |
| CHEMBL2205818 | — | — | 1 | 7.17 |
| CHEMBL2205836 | — | — | 1 | 7.16 |
| CHEMBL2205814 | — | — | 1 | 7.00 |
| CHEMBL2205823 | — | — | 1 | 6.72 |
| CHEMBL2205825 | — | — | 1 | 6.70 |
| CHEMBL2205827 | — | — | 1 | 6.64 |
| CHEMBL2205824 | — | — | 1 | 6.49 |
| CHEMBL1189234 | — | — | 1 | 6.47 |
| CHEMBL2205829 | — | — | 1 | 6.36 |
| CHEMBL2205828 | — | — | 1 | 6.21 |
| CHEMBL2205817 | — | — | 1 | 6.09 |
| CHEMBL2205832 | — | — | 1 | 5.98 |
| CHEMBL2205816 | — | — | 1 | 5.93 |
| CHEMBL2205834 | — | — | 1 | 5.82 |
| CHEMBL2205830 | — | — | 1 | 5.37 |
| CHEMBL2205833 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL408867 | [11C]SA4503 | Ki | = | 4.63 | nM | 8.33 |
| CHEMBL2205822 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL2205831 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2205821 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2205812 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL2205813 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2205820 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2205819 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2205815 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2205835 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2205811 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL2205826 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2205818 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2205836 | — | Ki | = | 68.7 | nM | 7.16 |
| CHEMBL2205814 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL2205823 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2205825 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2205827 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL2205824 | — | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL1189234 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL2205829 | — | Ki | = | 435.0 | nM | 6.36 |
| CHEMBL2205828 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL2205817 | — | Ki | = | 815.0 | nM | 6.09 |
| CHEMBL2205832 | — | Ki | = | 1048.0 | nM | 5.98 |
| CHEMBL2205816 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL2205834 | — | Ki | = | 1502.0 | nM | 5.82 |
| CHEMBL2205830 | — | Ki | = | 4289.0 | nM | 5.37 |
| CHEMBL2205833 | — | Ki | > | 10000.0 | nM | - |