Assay Detail
Binding
CHEMBL3388115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ENT1 expressed in porcine PK15NTD cells by cell-based [3H]5-uridine uptake assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PK15NTD |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.54 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353069 | — | — | 1 | 8.55 |
| CHEMBL3353072 | — | — | 1 | 8.49 |
| CHEMBL3353074 | — | — | 1 | 8.34 |
| CHEMBL126075 | DILAZEP | 2.0 | 1 | 7.76 |
| CHEMBL3353071 | — | — | 1 | 7.75 |
| CHEMBL3353073 | — | — | 1 | 7.51 |
| CHEMBL3353070 | — | — | 1 | 7.18 |
| CHEMBL3353077 | — | — | 1 | 7.03 |
| CHEMBL3353076 | — | — | 1 | 6.66 |
| CHEMBL3353075 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353069 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3353072 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3353074 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL126075 | DILAZEP | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL3353071 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL3353073 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3353070 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL3353077 | — | IC50 | = | 93.9 | nM | 7.03 |
| CHEMBL3353076 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL3353075 | — | IC50 | = | 803.0 | nM | 6.09 |