Assay Detail
Functional
CHEMBL873339
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Concentration required to kill human epidermoid KB-3-1 cell lines containing very low 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 | 8.66 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184019 | — | — | 1 | 9.64 |
| CHEMBL185151 | HEMIASTERLIN | — | 1 | 9.52 |
| CHEMBL186657 | — | — | 1 | 9.40 |
| CHEMBL182955 | — | — | 1 | 9.26 |
| CHEMBL365437 | — | — | 1 | 9.25 |
| CHEMBL186197 | — | — | 1 | 9.19 |
| CHEMBL366258 | — | — | 1 | 9.10 |
| CHEMBL359785 | — | — | 1 | 9.07 |
| CHEMBL363988 | — | — | 2 | 9.05 |
| CHEMBL182319 | TALTOBULIN | 2.0 | 1 | 9.00 |
| CHEMBL424988 | — | — | 1 | 9.00 |
| CHEMBL365407 | — | — | 1 | 8.94 |
| CHEMBL185969 | — | — | 1 | 8.82 |
| CHEMBL186812 | — | — | 1 | 8.74 |
| CHEMBL360836 | — | — | 1 | 8.72 |
| CHEMBL187085 | — | — | 1 | 8.72 |
| CHEMBL185530 | — | — | 1 | 8.70 |
| CHEMBL184350 | — | — | 1 | 8.68 |
| CHEMBL362723 | — | — | 1 | 8.21 |
| CHEMBL186152 | — | — | 1 | 8.10 |
| CHEMBL187214 | — | — | 1 | 8.04 |
| CHEMBL186809 | — | — | 1 | 7.77 |
| CHEMBL187129 | — | — | 1 | 7.77 |
| CHEMBL186967 | — | — | 1 | 7.66 |
| CHEMBL184978 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184019 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL185151 | HEMIASTERLIN | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL186657 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL182955 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL365437 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL186197 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL366258 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL359785 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL363988 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL182319 | TALTOBULIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL424988 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL365407 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL185969 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL186812 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL360836 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL187085 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL185530 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL184350 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL362723 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL363988 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL186152 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL187214 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL186809 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL187129 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL186967 | — | IC50 | = | 21.9 | nM | 7.66 |
| CHEMBL184978 | — | IC50 | = | 263.0 | nM | 6.58 |