Assay Detail
Functional
CHEMBL5209596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861)
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Equilibrative nucleoside transporter 1 (CHEMBL1997) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.74 | 10.00 |
| EC50 | 1 | 4.20 | 4.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL126075 | DILAZEP | 2.0 | 1 | 10.00 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | — | 1 | 8.59 |
| CHEMBL1628717 | DRAFLAZINE | 2.0 | 1 | 8.28 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 8.09 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL126075 | DILAZEP | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1628717 | DRAFLAZINE | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL477 | ADENOSINE | EC50 | = | 63000.0 | nM | 4.20 |