Assay Detail
Binding
CHEMBL924283
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Displacement of SAENTA-fluorescein from human ENT1 in K562 cells after 45 mins by flow cytometry
22
Total Activities
22
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 | Intermediate |
Target
Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel C2-purine position analogs of nitrobenzylmercaptopurine riboside as human equilibrative nucleoside transporter 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.32 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | — | 1 | 9.15 |
| CHEMBL394171 | — | — | 1 | 8.96 |
| CHEMBL239246 | — | — | 1 | 8.68 |
| CHEMBL393342 | — | — | 1 | 7.96 |
| CHEMBL239889 | — | — | 1 | 7.96 |
| CHEMBL239670 | — | — | 1 | 7.96 |
| CHEMBL391730 | — | — | 1 | 7.62 |
| CHEMBL394012 | — | — | 1 | 7.62 |
| CHEMBL391838 | — | — | 1 | 7.60 |
| CHEMBL239454 | — | — | 1 | 7.48 |
| CHEMBL240101 | — | — | 1 | 7.47 |
| CHEMBL239887 | — | — | 1 | 7.07 |
| CHEMBL393322 | — | — | 1 | 6.90 |
| CHEMBL239248 | — | — | 1 | 6.71 |
| CHEMBL391651 | — | — | 1 | 6.61 |
| CHEMBL239888 | — | — | 1 | 6.61 |
| CHEMBL240102 | — | — | 1 | 6.50 |
| CHEMBL393120 | — | — | 1 | 6.49 |
| CHEMBL239455 | — | — | 1 | 6.45 |
| CHEMBL428031 | — | — | 1 | 6.41 |
| CHEMBL239669 | — | — | 1 | 6.40 |
| CHEMBL239451 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL394171 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL239246 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL393342 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL239889 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL239670 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL391730 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL394012 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL391838 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL239454 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL240101 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL239887 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL393322 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL239248 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL391651 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL239888 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL240102 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL393120 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL239455 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL428031 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL239669 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL239451 | — | Ki | = | 429.0 | nM | 6.37 |