Assay Detail
Functional
CHEMBL827481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB 3-1 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: modification of the A segment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.23 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184019 | — | — | 1 | 9.19 |
| CHEMBL185151 | HEMIASTERLIN | — | 1 | 9.00 |
| CHEMBL186657 | — | — | 1 | 8.95 |
| CHEMBL182955 | — | — | 1 | 8.91 |
| CHEMBL365437 | — | — | 1 | 8.77 |
| CHEMBL186197 | — | — | 1 | 8.77 |
| CHEMBL363988 | — | — | 2 | 8.74 |
| CHEMBL424988 | — | — | 1 | 8.74 |
| CHEMBL366258 | — | — | 1 | 8.74 |
| CHEMBL359785 | — | — | 1 | 8.70 |
| CHEMBL182319 | TALTOBULIN | 2.0 | 1 | 8.62 |
| CHEMBL185969 | — | — | 1 | 8.59 |
| CHEMBL365407 | — | — | 1 | 8.49 |
| CHEMBL185530 | — | — | 1 | 8.41 |
| CHEMBL186812 | — | — | 1 | 8.39 |
| CHEMBL360836 | — | — | 1 | 8.27 |
| CHEMBL187085 | — | — | 1 | 8.24 |
| CHEMBL184350 | — | — | 1 | 8.18 |
| CHEMBL362723 | — | — | 1 | 7.79 |
| CHEMBL186809 | — | — | 1 | 7.72 |
| CHEMBL186152 | — | — | 1 | 7.70 |
| CHEMBL187214 | — | — | 1 | 7.62 |
| CHEMBL187129 | — | — | 1 | 7.56 |
| CHEMBL186967 | — | — | 1 | 6.28 |
| CHEMBL184978 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184019 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL185151 | HEMIASTERLIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL186657 | — | IC50 | = | 1.13 | nM | 8.95 |
| CHEMBL182955 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL365437 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL186197 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL363988 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL366258 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL424988 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL359785 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL182319 | TALTOBULIN | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL185969 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL365407 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL185530 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL186812 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL360836 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL187085 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL184350 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL363988 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL362723 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL186809 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL186152 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL187214 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL187129 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL186967 | — | IC50 | = | 525.3 | nM | 6.28 |
| CHEMBL184978 | — | IC50 | = | 1698.0 | nM | 5.77 |