Assay Detail
Functional
CHEMBL1687604
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against P-gp overexpressing human MES-SA/Dx5-Rx1 cells assessed as growth inhibition
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.10 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1683543 | — | — | 1 | 9.11 |
| CHEMBL1683539 | — | — | 1 | 8.93 |
| CHEMBL1683541 | — | — | 1 | 8.87 |
| CHEMBL1683537 | — | — | 1 | 8.83 |
| CHEMBL1683523 | — | — | 1 | 8.73 |
| CHEMBL1683534 | — | — | 1 | 8.73 |
| CHEMBL1683540 | — | — | 1 | 8.70 |
| CHEMBL1683530 | — | — | 1 | 8.65 |
| CHEMBL1683524 | — | — | 1 | 8.62 |
| CHEMBL1683525 | — | — | 1 | 8.56 |
| CHEMBL1683529 | — | — | 1 | 8.55 |
| CHEMBL1683542 | — | — | 1 | 8.54 |
| CHEMBL1683532 | — | — | 1 | 8.54 |
| CHEMBL1683531 | — | — | 1 | 8.46 |
| CHEMBL1683535 | — | — | 1 | 8.41 |
| CHEMBL1683528 | — | — | 1 | 8.38 |
| CHEMBL1683538 | — | — | 1 | 8.25 |
| CHEMBL1683522 | — | — | 1 | 8.19 |
| CHEMBL1683527 | — | — | 1 | 7.95 |
| CHEMBL1683526 | — | — | 1 | 7.64 |
| CHEMBL1683533 | — | — | 1 | 7.44 |
| CHEMBL1683536 | — | — | 1 | 7.02 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 6.36 |
| CHEMBL53463 | DOXORUBICIN | 4.0 | 1 | 5.57 |
| CHEMBL1683590 | ERIBULIN | 4.0 | 1 | 5.51 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1683543 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL1683539 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL1683541 | — | IC50 | = | 1.36 | nM | 8.87 |
| CHEMBL1683537 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL1683523 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL1683534 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL1683540 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL1683530 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL1683524 | — | IC50 | = | 2.38 | nM | 8.62 |
| CHEMBL1683525 | — | IC50 | = | 2.77 | nM | 8.56 |
| CHEMBL1683529 | — | IC50 | = | 2.82 | nM | 8.55 |
| CHEMBL1683542 | — | IC50 | = | 2.91 | nM | 8.54 |
| CHEMBL1683532 | — | IC50 | = | 2.92 | nM | 8.54 |
| CHEMBL1683531 | — | IC50 | = | 3.47 | nM | 8.46 |
| CHEMBL1683535 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1683528 | — | IC50 | = | 4.13 | nM | 8.38 |
| CHEMBL1683538 | — | IC50 | = | 5.67 | nM | 8.25 |
| CHEMBL1683522 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1683527 | — | IC50 | = | 11.32 | nM | 7.95 |
| CHEMBL1683526 | — | IC50 | = | 22.96 | nM | 7.64 |
| CHEMBL1683533 | — | IC50 | = | 36.66 | nM | 7.44 |
| CHEMBL1683536 | — | IC50 | = | 95.55 | nM | 7.02 |
| CHEMBL159 | VINBLASTINE | IC50 | = | 439.73 | nM | 6.36 |
| CHEMBL53463 | DOXORUBICIN | IC50 | = | 2702.33 | nM | 5.57 |
| CHEMBL1683590 | ERIBULIN | IC50 | = | 3058.0 | nM | 5.51 |
| CHEMBL428647 | PACLITAXEL | IC50 | > | 1000.0 | nM | - |