Assay Detail
Functional
CHEMBL5626767
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability by MTT assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Modulation of taxane binding to tubulin curved and straight conformations by systematic 3'N modification provides for improved microtubule binding, persistent cytotoxicity and in vivo potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.21 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633002 | — | — | 1 | 9.15 |
| CHEMBL92 | DOCETAXEL ANHYDROUS | 4.0 | 1 | 9.15 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 9.00 |
| CHEMBL5632990 | — | — | 1 | 8.96 |
| CHEMBL5633337 | — | — | 1 | 8.59 |
| CHEMBL5631317 | — | — | 1 | 8.52 |
| CHEMBL5631664 | — | — | 1 | 8.05 |
| CHEMBL5631846 | — | — | 1 | 7.24 |
| CHEMBL5632799 | — | — | 1 | 6.80 |
| CHEMBL5633877 | — | — | 1 | 6.70 |
| CHEMBL5632754 | — | — | 1 | 5.96 |
| CHEMBL5632054 | — | — | 1 | 5.85 |
| CHEMBL5633421 | — | — | 1 | 5.52 |
| CHEMBL5631718 | — | — | 1 | 5.40 |
| CHEMBL5633843 | — | — | 1 | 5.30 |
| CHEMBL5633260 | — | — | 1 | 5.16 |
| CHEMBL5631582 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633002 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL92 | DOCETAXEL ANHYDROUS | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5632990 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5633337 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5631317 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5631664 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5631846 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5632799 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5633877 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5632754 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5632054 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL5633421 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5631718 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5633843 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5633260 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL5631582 | — | IC50 | > | 25000.0 | nM | - |