Assay Detail
Binding
CHEMBL936365
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Displacement of 5-(SAENTA)-X8-fluorescein from human ENT1 transporter in human K562 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K562 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.86 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260570 | — | — | 1 | 9.35 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | — | 1 | 9.15 |
| CHEMBL261227 | — | — | 1 | 7.82 |
| CHEMBL438046 | — | — | 1 | 7.72 |
| CHEMBL408670 | — | — | 1 | 6.60 |
| CHEMBL261226 | — | — | 1 | 6.52 |
| CHEMBL258729 | — | — | 1 | - |
| CHEMBL259855 | — | — | 1 | - |
| CHEMBL260281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260570 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL261227 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL438046 | — | Ki | = | 18.89 | nM | 7.72 |
| CHEMBL408670 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL261226 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL258729 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL259855 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL260281 | — | Ki | > | 1000.0 | nM | - |