Assay Detail
Binding
CHEMBL809516
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Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.02 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303336 | — | — | 1 | 9.59 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.19 |
| CHEMBL64683 | — | — | 1 | 8.89 |
| CHEMBL60267 | — | — | 1 | 8.85 |
| CHEMBL59335 | — | — | 1 | 8.82 |
| CHEMBL304232 | — | — | 1 | 8.68 |
| CHEMBL59464 | — | — | 1 | 8.60 |
| CHEMBL42228 | — | — | 1 | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.52 |
| CHEMBL61343 | — | — | 1 | 8.52 |
| CHEMBL61747 | — | — | 1 | 8.35 |
| CHEMBL64113 | — | — | 1 | 8.28 |
| CHEMBL279586 | — | — | 1 | 8.25 |
| CHEMBL59249 | — | — | 1 | 8.24 |
| CHEMBL62137 | — | — | 1 | 8.15 |
| CHEMBL64344 | — | — | 1 | 8.12 |
| CHEMBL61812 | — | — | 1 | 8.11 |
| CHEMBL397705 | REL-PENTAZOCINE | — | 1 | 8.05 |
| CHEMBL60845 | — | — | 1 | 8.00 |
| CHEMBL59273 | — | — | 1 | 8.00 |
| CHEMBL59940 | — | — | 1 | 7.85 |
| CHEMBL64302 | — | — | 1 | 7.85 |
| CHEMBL59306 | — | — | 1 | 7.85 |
| CHEMBL62188 | — | — | 1 | 7.82 |
| CHEMBL61539 | — | — | 1 | 7.80 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.77 |
| CHEMBL433831 | — | — | 1 | 7.57 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.44 |
| CHEMBL303804 | — | — | 1 | 7.36 |
| CHEMBL60859 | BMY-14802 | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303336 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL64683 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL60267 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL59335 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL304232 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL59464 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL42228 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL60542 | (+)-PENTAZOCINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL61343 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL61747 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL64113 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL279586 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL59249 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL62137 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL64344 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL61812 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL397705 | REL-PENTAZOCINE | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL60845 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL59273 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL59940 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL64302 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL59306 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL62188 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL61539 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL61479 | SIRAMESINE | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL433831 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL282433 | DITOLYLGUANIDINE | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL303804 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL416506 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL62994 | — | IC50 | = | 1200.0 | nM | 5.92 |