Assay Detail
Binding
CHEMBL2050136
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Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate after 120 mins by liquid scintillation counting in presence of (+)-pentazocine
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.12 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20730 | VESAMICOL | — | 1 | 6.46 |
| CHEMBL2047120 | — | — | 1 | 5.86 |
| CHEMBL2047127 | — | — | 1 | 5.59 |
| CHEMBL2047122 | — | — | 1 | 5.40 |
| CHEMBL2047124 | — | — | 1 | 5.40 |
| CHEMBL2047126 | — | — | 1 | 5.38 |
| CHEMBL2047232 | — | — | 1 | 5.31 |
| CHEMBL2047234 | — | — | 1 | 5.20 |
| CHEMBL2047238 | — | — | 1 | 5.11 |
| CHEMBL2047239 | — | — | 1 | 5.01 |
| CHEMBL2047237 | — | — | 1 | 4.91 |
| CHEMBL2047123 | — | — | 1 | 4.81 |
| CHEMBL2047125 | — | — | 1 | 4.79 |
| CHEMBL2047240 | — | — | 1 | 4.69 |
| CHEMBL2047236 | — | — | 1 | 4.68 |
| CHEMBL2047235 | — | — | 1 | 4.61 |
| CHEMBL2047233 | — | — | 1 | 4.61 |
| CHEMBL2047128 | — | — | 1 | 4.39 |
| CHEMBL2047121 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20730 | VESAMICOL | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL2047120 | — | Ki | = | 1375.0 | nM | 5.86 |
| CHEMBL2047127 | — | Ki | = | 2590.0 | nM | 5.59 |
| CHEMBL2047122 | — | Ki | = | 3950.0 | nM | 5.40 |
| CHEMBL2047124 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL2047126 | — | Ki | = | 4220.0 | nM | 5.38 |
| CHEMBL2047232 | — | Ki | = | 4850.0 | nM | 5.31 |
| CHEMBL2047234 | — | Ki | = | 6380.0 | nM | 5.20 |
| CHEMBL2047238 | — | Ki | = | 7830.0 | nM | 5.11 |
| CHEMBL2047239 | — | Ki | = | 9709.0 | nM | 5.01 |
| CHEMBL2047237 | — | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL2047123 | — | Ki | = | 15500.0 | nM | 4.81 |
| CHEMBL2047125 | — | Ki | = | 16400.0 | nM | 4.79 |
| CHEMBL2047240 | — | Ki | = | 20500.0 | nM | 4.69 |
| CHEMBL2047236 | — | Ki | = | 20700.0 | nM | 4.68 |
| CHEMBL2047235 | — | Ki | = | 24400.0 | nM | 4.61 |
| CHEMBL2047233 | — | Ki | = | 24300.0 | nM | 4.61 |
| CHEMBL2047128 | — | Ki | = | 40400.0 | nM | 4.39 |
| CHEMBL2047121 | — | Ki | > | 10000.0 | nM | - |