Assay Detail
Binding
CHEMBL5339617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ditolylguanidine from sigma 2 receptor/TMEM97 in rat PC-12 cells assessed as inhibition constant in the presence of (+)-pentazocine by competition binding assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | PC-12 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Targeting σ<sub>2</sub>R/TMEM97 with novel aminotetralins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.83 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5438672 | — | — | 1 | 8.68 |
| CHEMBL5401174 | — | — | 1 | 8.68 |
| CHEMBL5401938 | — | — | 1 | 8.57 |
| CHEMBL5394787 | — | — | 1 | 8.35 |
| CHEMBL5393862 | — | — | 1 | 8.34 |
| CHEMBL5175530 | — | — | 1 | 8.29 |
| CHEMBL5403404 | — | — | 1 | 8.26 |
| CHEMBL5438518 | — | — | 1 | 8.14 |
| CHEMBL5395472 | — | — | 1 | 8.08 |
| CHEMBL5422903 | — | — | 1 | 8.03 |
| CHEMBL5437307 | — | — | 1 | 7.92 |
| CHEMBL5406262 | — | — | 1 | 7.89 |
| CHEMBL5423167 | — | — | 1 | 7.78 |
| CHEMBL5440859 | — | — | 1 | 7.70 |
| CHEMBL5408800 | — | — | 1 | 7.68 |
| CHEMBL5411467 | — | — | 1 | 7.60 |
| CHEMBL5400163 | — | — | 1 | 7.58 |
| CHEMBL5397633 | — | — | 1 | 7.46 |
| CHEMBL5189158 | — | — | 1 | 7.34 |
| CHEMBL5427018 | — | — | 1 | 7.30 |
| CHEMBL5419932 | — | — | 1 | 6.55 |
| CHEMBL5418564 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5438672 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5401174 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5401938 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5394787 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5393862 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5175530 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL5403404 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5438518 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL5395472 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL5422903 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL5437307 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5406262 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5423167 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL5440859 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5408800 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5411467 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL5400163 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5397633 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5189158 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL5427018 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL5419932 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL5418564 | — | Ki | = | 894.0 | nM | 6.05 |