Assay Detail
Binding
CHEMBL2050134
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Displacement of [3H]vesamicol from human VAChT expressed in rat PC12 cells after 24 hrs by liquid scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-12 |
| Confidence | 9 — Direct single protein target |
| 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 | 6.60 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2047236 | — | — | 1 | 7.99 |
| CHEMBL2047126 | — | — | 1 | 7.94 |
| CHEMBL20730 | VESAMICOL | — | 1 | 7.82 |
| CHEMBL2047232 | — | — | 1 | 7.81 |
| CHEMBL2047234 | — | — | 1 | 7.72 |
| CHEMBL2047122 | — | — | 1 | 7.20 |
| CHEMBL2047233 | — | — | 1 | 6.95 |
| CHEMBL2047124 | — | — | 1 | 6.91 |
| CHEMBL2047235 | — | — | 1 | 6.85 |
| CHEMBL2047239 | — | — | 1 | 6.69 |
| CHEMBL2047127 | — | — | 1 | 6.63 |
| CHEMBL2047123 | — | — | 1 | 6.09 |
| CHEMBL2047125 | — | — | 1 | 5.92 |
| CHEMBL2047237 | — | — | 1 | 5.89 |
| CHEMBL2047240 | — | — | 1 | 5.87 |
| CHEMBL2047238 | — | — | 1 | 5.70 |
| CHEMBL2047128 | — | — | 1 | 5.52 |
| CHEMBL2047120 | — | — | 1 | 5.06 |
| CHEMBL2047121 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2047236 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL2047126 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL20730 | VESAMICOL | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL2047232 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL2047234 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2047122 | — | Ki | = | 62.7 | nM | 7.20 |
| CHEMBL2047233 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL2047124 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL2047235 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL2047239 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL2047127 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL2047123 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL2047125 | — | Ki | = | 1190.0 | nM | 5.92 |
| CHEMBL2047237 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL2047240 | — | Ki | = | 1350.0 | nM | 5.87 |
| CHEMBL2047238 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL2047128 | — | Ki | = | 3020.0 | nM | 5.52 |
| CHEMBL2047120 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL2047121 | — | Ki | = | 13000.0 | nM | 4.89 |