Assay Detail
Binding
CHEMBL5164051
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 human HEK293T cells assessed as inhibition constant in presence of (+)-pentazocine by radioligand competition binding assay
30
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.25 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175530 | — | — | 2 | 8.10 |
| CHEMBL5208940 | — | — | 2 | 7.85 |
| CHEMBL5206383 | — | — | 2 | 7.85 |
| CHEMBL5185602 | — | — | 2 | 7.72 |
| CHEMBL5177703 | — | — | 2 | 7.70 |
| CHEMBL5189334 | — | — | 2 | 7.50 |
| CHEMBL5183680 | — | — | 2 | 7.42 |
| CHEMBL5207336 | — | — | 2 | 7.29 |
| CHEMBL5191108 | — | — | 2 | 7.20 |
| CHEMBL5197224 | — | — | 2 | 7.12 |
| CHEMBL5170591 | — | — | 2 | 7.10 |
| CHEMBL5184025 | — | — | 2 | 7.05 |
| CHEMBL5182001 | — | — | 2 | 6.31 |
| CHEMBL5189037 | — | — | 2 | 6.27 |
| CHEMBL5181506 | — | — | 2 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175530 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL5175530 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL5208940 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL5206383 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5208940 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5206383 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL5185602 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5185602 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL5177703 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL5177703 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5189334 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5189334 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL5183680 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5183680 | — | Ki | = | 38.02 | nM | 7.42 |
| CHEMBL5207336 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL5207336 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL5191108 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL5191108 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL5197224 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL5197224 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL5170591 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL5170591 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL5184025 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL5184025 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL5182001 | — | Ki | = | 491.0 | nM | 6.31 |
| CHEMBL5182001 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL5189037 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL5189037 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL5181506 | — | Ki | = | 549.54 | nM | 6.26 |
| CHEMBL5181506 | — | Ki | = | 554.0 | nM | 6.26 |