Assay Detail
Functional
CHEMBL2077068
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
ATP-binding cassette sub-family C member 4 (CHEMBL1743128) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.87 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 5.70 |
| CHEMBL285913 | TREQUINSIN | 2.0 | 1 | 5.00 |
| CHEMBL15177 | MK-571 | — | 1 | 5.00 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 4.70 |
| CHEMBL126075 | DILAZEP | 2.0 | 1 | 4.70 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL285913 | TREQUINSIN | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL15177 | MK-571 | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL126075 | DILAZEP | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL418509 | NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE | IC50 | = | 75000.0 | nM | 4.12 |