Assay Detail
Functional
CHEMBL832419
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Compound was tested for cytotoxicity against paclitaxel resistant KB-8-5 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 |
| 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 | 6.96 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | 2.0 | 1 | 8.64 |
| CHEMBL182217 | — | — | 1 | 8.21 |
| CHEMBL184111 | — | — | 1 | 8.21 |
| CHEMBL182909 | — | — | 1 | 8.14 |
| CHEMBL183955 | — | — | 1 | 8.00 |
| CHEMBL362263 | — | — | 1 | 7.82 |
| CHEMBL361536 | — | — | 1 | 7.80 |
| CHEMBL185336 | — | — | 1 | 7.77 |
| CHEMBL181429 | — | — | 1 | 7.77 |
| CHEMBL184932 | — | — | 1 | 7.72 |
| CHEMBL185381 | — | — | 1 | 7.68 |
| CHEMBL182422 | — | — | 1 | 7.66 |
| CHEMBL363927 | — | — | 1 | 7.29 |
| CHEMBL427143 | — | — | 1 | 7.28 |
| CHEMBL360879 | — | — | 1 | 7.28 |
| CHEMBL185116 | — | — | 1 | 7.24 |
| CHEMBL182289 | — | — | 1 | 7.17 |
| CHEMBL359700 | — | — | 1 | 6.94 |
| CHEMBL182912 | — | — | 1 | 6.76 |
| CHEMBL183487 | — | — | 1 | 6.75 |
| CHEMBL361738 | — | — | 1 | 6.74 |
| CHEMBL360556 | — | — | 1 | 6.73 |
| CHEMBL443043 | — | — | 1 | 6.69 |
| CHEMBL183385 | — | — | 1 | 6.57 |
| CHEMBL185508 | — | — | 1 | 6.35 |
| CHEMBL182669 | — | — | 1 | 6.35 |
| CHEMBL183401 | — | — | 1 | 6.32 |
| CHEMBL183477 | — | — | 1 | 6.29 |
| CHEMBL182619 | — | — | 1 | 6.25 |
| CHEMBL182063 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182319 | TALTOBULIN | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL182217 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL184111 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL182909 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL183955 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL362263 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL361536 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL185336 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL181429 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL184932 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL185381 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL182422 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL363927 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL427143 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL360879 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL185116 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL182289 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL359700 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL182912 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL183487 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL361738 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL360556 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL443043 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL183385 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL185508 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL182669 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL183401 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL183477 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL182619 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL182063 | — | IC50 | = | 599.0 | nM | 6.22 |
| CHEMBL185218 | — | IC50 | = | 664.0 | nM | 6.18 |
| CHEMBL182395 | — | IC50 | = | 1326.0 | nM | 5.88 |
| CHEMBL185242 | — | IC50 | = | 1364.0 | nM | 5.87 |
| CHEMBL182985 | — | IC50 | = | 1577.0 | nM | 5.80 |
| CHEMBL185185 | — | IC50 | = | 1738.0 | nM | 5.76 |
| CHEMBL426787 | — | IC50 | = | 1819.0 | nM | 5.74 |
| CHEMBL363674 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL183593 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL183063 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL361010 | — | IC50 | > | 3000.0 | nM | - |