Assay Detail
Binding
CHEMBL803878
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for sigma opioid receptor using [3H](+)-3-PPP as radioligand
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.32 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2303661 | — | — | 1 | 8.70 |
| CHEMBL607449 | — | — | 1 | 7.92 |
| CHEMBL606937 | — | — | 1 | 7.43 |
| CHEMBL607212 | — | — | 1 | 7.38 |
| CHEMBL607333 | — | — | 1 | 7.12 |
| CHEMBL607332 | — | — | 1 | 7.11 |
| CHEMBL607275 | — | — | 1 | 6.96 |
| CHEMBL607278 | — | — | 1 | 6.90 |
| CHEMBL607210 | — | — | 1 | 6.89 |
| CHEMBL301867 | — | — | 1 | 6.71 |
| CHEMBL607451 | — | — | 1 | 6.71 |
| CHEMBL607273 | — | — | 1 | 6.70 |
| CHEMBL606784 | — | — | 1 | 6.68 |
| CHEMBL606834 | — | — | 1 | 6.68 |
| CHEMBL607390 | — | — | 1 | 6.65 |
| CHEMBL607274 | — | — | 1 | 6.64 |
| CHEMBL607450 | — | — | 1 | 6.56 |
| CHEMBL607448 | — | — | 1 | 6.52 |
| CHEMBL606889 | — | — | 1 | 6.38 |
| CHEMBL607335 | — | — | 1 | 6.06 |
| CHEMBL607156 | — | — | 1 | 6.03 |
| CHEMBL2374421 | — | — | 1 | 6.01 |
| CHEMBL607391 | — | — | 1 | 5.94 |
| CHEMBL607157 | — | — | 1 | 5.90 |
| CHEMBL607214 | — | — | 1 | 5.88 |
| CHEMBL606783 | — | — | 1 | 5.86 |
| CHEMBL606887 | — | — | 1 | 5.82 |
| CHEMBL607392 | — | — | 1 | 5.79 |
| CHEMBL606838 | — | — | 1 | 5.68 |
| CHEMBL606835 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2303661 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL607449 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL606937 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL607212 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL607333 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL607332 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL607275 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL607278 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL607210 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL301867 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL607451 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL607273 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL606784 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL606834 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL607390 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL607274 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL607450 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL607448 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL606889 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL607335 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL607156 | — | IC50 | = | 928.0 | nM | 6.03 |
| CHEMBL2374421 | — | IC50 | = | 966.0 | nM | 6.01 |
| CHEMBL607391 | — | IC50 | = | 1155.0 | nM | 5.94 |
| CHEMBL607157 | — | IC50 | = | 1247.0 | nM | 5.90 |
| CHEMBL607214 | — | IC50 | = | 1335.0 | nM | 5.88 |
| CHEMBL606783 | — | IC50 | = | 1385.0 | nM | 5.86 |
| CHEMBL606887 | — | IC50 | = | 1516.0 | nM | 5.82 |
| CHEMBL607392 | — | IC50 | = | 1609.0 | nM | 5.79 |
| CHEMBL606838 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL606835 | — | IC50 | = | 2374.0 | nM | 5.62 |
| CHEMBL606891 | — | IC50 | = | 2593.0 | nM | 5.59 |
| CHEMBL607213 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL607211 | — | IC50 | = | 3267.0 | nM | 5.49 |
| CHEMBL607158 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL607159 | — | IC50 | = | 5303.0 | nM | 5.28 |
| CHEMBL607452 | — | IC50 | = | 5952.0 | nM | 5.22 |
| CHEMBL606890 | — | IC50 | = | 6058.0 | nM | 5.22 |
| CHEMBL607276 | — | IC50 | = | 7551.0 | nM | 5.12 |