Assay Detail
Binding
CHEMBL5339633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ditolylguanidine from human sigma 2 receptor/TMEM97 transfected in HEK293 cells assessed as inhibition constant in the presence of (+)-pentazocine by competition binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting σ<sub>2</sub>R/TMEM97 with novel aminotetralins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.48 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5421620 | — | — | 1 | 8.02 |
| CHEMBL5415235 | — | — | 1 | 7.82 |
| CHEMBL5408937 | — | — | 1 | 7.77 |
| CHEMBL5423845 | — | — | 1 | 7.77 |
| CHEMBL5403404 | — | — | 1 | 7.48 |
| CHEMBL5419308 | — | — | 1 | 7.46 |
| CHEMBL5439058 | — | — | 1 | 7.28 |
| CHEMBL5402989 | — | — | 1 | 6.89 |
| CHEMBL5439530 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5421620 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL5415235 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5408937 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5423845 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5403404 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5419308 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5439058 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL5402989 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL5439530 | — | Ki | = | 135.0 | nM | 6.87 |