Assay Detail
ADMET
CHEMBL3528993
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Binding affinity to recombinant human CNT2 expressed in Saccharomyces cerevisiae assessed as inhibition of [3H]-uridine transport after 15 mins by scintillation counting analysis
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 4.90 | 5.28 |
| IC50 | 3 | 4.88 | 5.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477 | ADENOSINE | 4.0 | 2 | 5.28 |
| CHEMBL100259 | URIDINE | 3.0 | 2 | 4.51 |
| CHEMBL392149 | TECADENOSON | 2.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477 | ADENOSINE | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL477 | ADENOSINE | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL100259 | URIDINE | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL100259 | URIDINE | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL392149 | TECADENOSON | Ki | = | 231000.0 | nM | - |
| CHEMBL392149 | TECADENOSON | IC50 | = | 239000.0 | nM | - |