Assay Detail
Functional
CHEMBL2078565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.055 uM) in membrane vesicles from Mrp2-expressing Sf9 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | Sf9 |
| Subcellular | Membrane vesicle |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
ATP-binding cassette sub-family C member 2 (CHEMBL2073676) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Charged amino acids in the transmembrane domains are involved in the determination of the substrate specificity of rat Mrp2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.29 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495936 | LEUKOTRIEN C4 | — | 1 | 6.19 |
| CHEMBL15177 | MK-571 | — | 1 | 5.58 |
| CHEMBL288943 | LEUKOTRIENE D4 | -1.0 | 1 | 5.26 |
| CHEMBL509456 | LEUKOTRIEN E4 | — | 1 | 5.01 |
| CHEMBL2074920 | LEUKOTRIEN F4 | — | 1 | 5.00 |
| CHEMBL213947 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495936 | LEUKOTRIEN C4 | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL15177 | MK-571 | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL288943 | LEUKOTRIENE D4 | IC50 | = | 5480.0 | nM | 5.26 |
| CHEMBL509456 | LEUKOTRIEN E4 | IC50 | = | 9830.0 | nM | 5.01 |
| CHEMBL2074920 | LEUKOTRIEN F4 | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL213947 | — | IC50 | = | 19300.0 | nM | 4.71 |