Assay Detail
Binding
CHEMBL5324504
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Displacement of [3H]-1,3-di-O-tolylguanidine from human sigma 2 receptor/TMEM97 transfected in sigma 1 receptor knockout HEK293 cell membranes assessed as inhibition constant measured after 120 mins by microbeta scintillation counting analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of WLB-89462, a New Drug-like and Highly Selective σ<sub>2</sub> Receptor Ligand with Neuroprotective Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.35 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5418939 | — | — | 1 | 9.00 |
| CHEMBL5395523 | — | — | 1 | 9.00 |
| CHEMBL5393813 | — | — | 1 | 8.52 |
| CHEMBL5425053 | — | — | 1 | 8.40 |
| CHEMBL4846092 | — | — | 1 | 8.30 |
| CHEMBL5418322 | — | — | 1 | 8.30 |
| CHEMBL5427726 | — | — | 1 | 8.22 |
| CHEMBL5401020 | — | — | 1 | 7.89 |
| CHEMBL5424034 | — | — | 1 | 7.42 |
| CHEMBL5394618 | — | — | 1 | 7.33 |
| CHEMBL5398618 | — | — | 1 | 7.23 |
| CHEMBL5400448 | — | — | 1 | 7.21 |
| CHEMBL5426449 | — | — | 1 | 7.21 |
| CHEMBL5426097 | — | — | 1 | 7.01 |
| CHEMBL5433551 | — | — | 1 | 6.94 |
| CHEMBL5438422 | — | — | 1 | 6.88 |
| CHEMBL5395314 | — | — | 1 | 6.79 |
| CHEMBL5395635 | — | — | 1 | 6.50 |
| CHEMBL5419738 | — | — | 1 | 6.34 |
| CHEMBL5416073 | — | — | 1 | 6.30 |
| CHEMBL5430674 | — | — | 1 | 6.14 |
| CHEMBL5435310 | — | — | 1 | 6.10 |
| CHEMBL5411022 | — | — | 1 | 6.02 |
| CHEMBL5400873 | — | — | 1 | - |
| CHEMBL5394360 | — | — | 1 | - |
| CHEMBL5432378 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5418939 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5395523 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5393813 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5425053 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4846092 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5418322 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5427726 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5401020 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5424034 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5394618 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5398618 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5400448 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL5426449 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL5426097 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL5433551 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL5438422 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL5395314 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL5395635 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL5419738 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL5416073 | — | Ki | = | 496.0 | nM | 6.30 |
| CHEMBL5430674 | — | Ki | = | 727.0 | nM | 6.14 |
| CHEMBL5435310 | — | Ki | = | 788.0 | nM | 6.10 |
| CHEMBL5411022 | — | Ki | = | 951.0 | nM | 6.02 |
| CHEMBL5400873 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5394360 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5432378 | — | Ki | > | 1000.0 | nM | - |