Assay Detail
ADMET
CHEMBL4699780
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Substrate activity at ENT1 in human BXPC-3 cells assessed as inhibition of cell growth pretreated with ENT1 inhibitor nitrobenzylthioinosine for 5 mins measured after 72 hrs by SRB assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | BXPC-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.50 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL888 | GEMCITABINE | 4.0 | 1 | 6.72 |
| CHEMBL4800221 | — | — | 1 | 6.42 |
| CHEMBL4796317 | — | — | 1 | 6.42 |
| CHEMBL4764619 | — | — | 1 | 6.42 |
| CHEMBL4749693 | — | — | 1 | - |
| CHEMBL4778383 | — | — | 1 | - |
| CHEMBL4746302 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL888 | GEMCITABINE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4800221 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4796317 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL4764619 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL4749693 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4778383 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4746302 | — | IC50 | > | 1000.0 | nM | - |