Assay Detail
Binding
CHEMBL3757559
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Inhibition of ASCT2-mediated glutamine transport in human HEK293 cells using [3H]-glutamine after 15 mins by scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neutral amino acid transporter B(0) (CHEMBL3562162) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 4.62 | 5.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3754498 | — | — | 1 | 5.14 |
| CHEMBL3752210 | — | — | 1 | 5.10 |
| CHEMBL3754053 | — | — | 1 | 5.02 |
| CHEMBL3752483 | — | — | 1 | 4.94 |
| CHEMBL3753592 | — | — | 1 | 4.92 |
| CHEMBL3754059 | — | — | 1 | 4.86 |
| CHEMBL3753993 | — | — | 1 | 4.76 |
| CHEMBL3753404 | — | — | 1 | 4.75 |
| CHEMBL3753173 | — | — | 1 | 4.59 |
| CHEMBL3752943 | — | — | 1 | 4.58 |
| CHEMBL3752249 | — | — | 1 | 4.47 |
| CHEMBL3754369 | — | — | 1 | 4.47 |
| CHEMBL3752316 | — | — | 1 | 4.40 |
| CHEMBL3752103 | — | — | 1 | 4.32 |
| CHEMBL3753808 | — | — | 1 | 4.29 |
| CHEMBL3753869 | — | — | 1 | 4.24 |
| CHEMBL3752494 | — | — | 1 | 4.22 |
| CHEMBL3754415 | — | — | 1 | 4.16 |
| CHEMBL6251 | — | — | 1 | - |
| CHEMBL3752700 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3754498 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3752210 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3754053 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3752483 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL3753592 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL3754059 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL3753993 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL3753404 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL3753173 | — | IC50 | = | 25600.0 | nM | 4.59 |
| CHEMBL3752943 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3752249 | — | IC50 | = | 33800.0 | nM | 4.47 |
| CHEMBL3754369 | — | IC50 | = | 33700.0 | nM | 4.47 |
| CHEMBL3752316 | — | IC50 | = | 40100.0 | nM | 4.40 |
| CHEMBL3752103 | — | IC50 | = | 48300.0 | nM | 4.32 |
| CHEMBL3753808 | — | IC50 | = | 50800.0 | nM | 4.29 |
| CHEMBL3753869 | — | IC50 | = | 57200.0 | nM | 4.24 |
| CHEMBL3752494 | — | IC50 | = | 59600.0 | nM | 4.22 |
| CHEMBL3754415 | — | IC50 | = | 69100.0 | nM | 4.16 |
| CHEMBL6251 | — | IC50 | = | 1200000.0 | nM | - |
| CHEMBL3752700 | — | IC50 | = | 141700.0 | nM | - |