Assay Detail
Binding
CHEMBL5628368
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Inhibition of MDR1 (unknown origin) overexpressed in MDCK cells using Calcein-AM as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence based assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrazole and oxadiazole derivatives as bioisosteres of tariquidar and elacridar: New potent P-gp modulators acting as MDR reversers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.94 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5631325 | — | — | 1 | 8.70 |
| CHEMBL5631270 | — | — | 1 | 8.52 |
| CHEMBL5632630 | — | — | 1 | 7.92 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 7.85 |
| CHEMBL5633719 | — | — | 1 | 7.72 |
| CHEMBL5633825 | — | — | 1 | 7.62 |
| CHEMBL5633373 | — | — | 1 | 7.39 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.36 |
| CHEMBL5631361 | — | — | 1 | 7.34 |
| CHEMBL5632739 | — | — | 1 | 7.15 |
| CHEMBL5633244 | — | — | 1 | 7.09 |
| CHEMBL5632579 | — | — | 1 | 7.05 |
| CHEMBL5633295 | — | — | 1 | 6.85 |
| CHEMBL5634029 | — | — | 1 | 6.58 |
| CHEMBL5633008 | — | — | 1 | 6.58 |
| CHEMBL5631377 | — | — | 1 | 6.40 |
| CHEMBL5632763 | — | — | 1 | 6.36 |
| CHEMBL5632163 | — | — | 1 | 6.26 |
| CHEMBL5632228 | — | — | 1 | 6.20 |
| CHEMBL5632419 | — | — | 1 | 6.12 |
| CHEMBL5633566 | — | — | 1 | 6.12 |
| CHEMBL5633240 | — | — | 1 | 6.02 |
| CHEMBL5632985 | — | — | 1 | 5.97 |
| CHEMBL5631869 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5631325 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5631270 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5632630 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL396298 | ELACRIDAR | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5633719 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5633825 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5633373 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL348475 | TARIQUIDAR | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5631361 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5632739 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5633244 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5632579 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5633295 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5634029 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5633008 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5631377 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5632763 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5632163 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5632228 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5632419 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5633566 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5633240 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5632985 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL5631869 | — | EC50 | = | 5270.0 | nM | 5.28 |