Assay Detail
Functional
CHEMBL833223
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Compound was tested for cytotoxicity against paclitaxel resistant KB-V1 cell line expressing P-glycoprotein
40
Total Activities
40
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
D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.18 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | 2.0 | 1 | 7.11 |
| CHEMBL185336 | — | — | 1 | 6.82 |
| CHEMBL182422 | — | — | 1 | 6.72 |
| CHEMBL183955 | — | — | 1 | 6.64 |
| CHEMBL181429 | — | — | 1 | 6.57 |
| CHEMBL184111 | — | — | 1 | 6.56 |
| CHEMBL182909 | — | — | 1 | 6.54 |
| CHEMBL182217 | — | — | 1 | 6.44 |
| CHEMBL362263 | — | — | 1 | 6.44 |
| CHEMBL184932 | — | — | 1 | 6.44 |
| CHEMBL361536 | — | — | 1 | 6.31 |
| CHEMBL360556 | — | — | 1 | 6.20 |
| CHEMBL363927 | — | — | 1 | 5.96 |
| CHEMBL182289 | — | — | 1 | 5.95 |
| CHEMBL182912 | — | — | 1 | 5.84 |
| CHEMBL427143 | — | — | 1 | 5.81 |
| CHEMBL360879 | — | — | 1 | 5.80 |
| CHEMBL182669 | — | — | 1 | 5.80 |
| CHEMBL185508 | — | — | 1 | 5.80 |
| CHEMBL185381 | — | — | 1 | 5.78 |
| CHEMBL182619 | — | — | 1 | 5.75 |
| CHEMBL182395 | — | — | 1 | 5.74 |
| CHEMBL185218 | — | — | 1 | 5.63 |
| CHEMBL185116 | — | — | 1 | 5.58 |
| CHEMBL183401 | — | — | 1 | - |
| CHEMBL182985 | — | — | 1 | - |
| CHEMBL443043 | — | — | 1 | - |
| CHEMBL359700 | — | — | 1 | - |
| CHEMBL361010 | — | — | 1 | - |
| CHEMBL183385 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL185336 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL182422 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL183955 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL181429 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL184111 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL182909 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL182217 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL362263 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL184932 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL361536 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL360556 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL363927 | — | IC50 | = | 1099.0 | nM | 5.96 |
| CHEMBL182289 | — | IC50 | = | 1134.0 | nM | 5.95 |
| CHEMBL182912 | — | IC50 | = | 1455.0 | nM | 5.84 |
| CHEMBL427143 | — | IC50 | = | 1533.0 | nM | 5.81 |
| CHEMBL360879 | — | IC50 | = | 1582.0 | nM | 5.80 |
| CHEMBL182669 | — | IC50 | = | 1594.0 | nM | 5.80 |
| CHEMBL185508 | — | IC50 | = | 1594.0 | nM | 5.80 |
| CHEMBL185381 | — | IC50 | = | 1673.0 | nM | 5.78 |
| CHEMBL182619 | — | IC50 | = | 1787.0 | nM | 5.75 |
| CHEMBL182395 | — | IC50 | = | 1805.0 | nM | 5.74 |
| CHEMBL185218 | — | IC50 | = | 2358.0 | nM | 5.63 |
| CHEMBL185116 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL185242 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183477 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183487 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL182063 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL185185 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL363674 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL426787 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183593 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL361738 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183063 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183385 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL361010 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL359700 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL443043 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL182985 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183401 | — | IC50 | > | 3000.0 | nM | - |