Assay Detail
Binding
CHEMBL3240359
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Inhibition of rat brain VGLUT assessed as inhibition of [3H]glutamate uptake into vesicles after 10 mins by scintillation spectrophotometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of small-azo-dyes as potent Vesicular Glutamate Transporters inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.70 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1640 | TRYPAN BLUE | 4.0 | 1 | 7.30 |
| CHEMBL1200712 | EVANS BLUE | 4.0 | 1 | 7.06 |
| CHEMBL3238498 | — | — | 1 | 5.80 |
| CHEMBL3238500 | — | — | 1 | 5.75 |
| CHEMBL3238484 | — | — | 1 | 5.68 |
| CHEMBL3238491 | — | — | 1 | 5.68 |
| CHEMBL311909 | CHICAGO SKY BLUE | — | 1 | 5.52 |
| CHEMBL3238501 | — | — | 1 | 5.48 |
| CHEMBL3238499 | — | — | 1 | 5.32 |
| CHEMBL3238488 | — | — | 1 | 5.24 |
| CHEMBL3238480 | — | — | 1 | 5.17 |
| CHEMBL76124 | — | — | 1 | 4.40 |
| CHEMBL3238490 | — | — | 1 | - |
| CHEMBL72332 | — | — | 1 | - |
| CHEMBL3238492 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1640 | TRYPAN BLUE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1200712 | EVANS BLUE | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3238498 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3238500 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3238484 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3238491 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL311909 | CHICAGO SKY BLUE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3238501 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3238499 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3238488 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3238480 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL76124 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3238490 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL72332 | — | IC50 | = | 286000.0 | nM | - |
| CHEMBL3238492 | — | IC50 | = | 288000.0 | nM | - |