Assay Detail
Functional
CHEMBL4254600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 6.62 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4285846 | — | — | 1 | 8.52 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 8.52 |
| CHEMBL67 | COMBRETASTATIN A4 | -1.0 | 1 | 8.10 |
| CHEMBL4285810 | — | — | 1 | 8.00 |
| CHEMBL4293724 | — | — | 1 | 7.80 |
| CHEMBL4290690 | — | — | 1 | 7.77 |
| CHEMBL4287325 | — | — | 1 | 7.57 |
| CHEMBL4283697 | — | — | 1 | 7.55 |
| CHEMBL4290051 | — | — | 1 | 7.55 |
| CHEMBL4285231 | — | — | 1 | 7.51 |
| CHEMBL4280283 | — | — | 1 | 7.47 |
| CHEMBL4289671 | — | — | 1 | 7.40 |
| CHEMBL4284722 | — | — | 1 | 7.33 |
| CHEMBL4292908 | — | — | 1 | 7.33 |
| CHEMBL4282802 | — | — | 1 | 7.20 |
| CHEMBL4277874 | — | — | 1 | 6.99 |
| CHEMBL4276677 | — | — | 1 | 6.97 |
| CHEMBL4286254 | — | — | 1 | 6.95 |
| CHEMBL4289588 | — | — | 1 | 6.90 |
| CHEMBL4290325 | — | — | 1 | 6.88 |
| CHEMBL4289248 | — | — | 1 | 6.74 |
| CHEMBL4277924 | — | — | 1 | 6.71 |
| CHEMBL4286914 | — | — | 1 | 6.62 |
| CHEMBL4278308 | — | — | 1 | 6.59 |
| CHEMBL4285297 | — | — | 1 | 6.42 |
| CHEMBL4281794 | — | — | 1 | 6.29 |
| CHEMBL4285778 | — | — | 1 | 6.25 |
| CHEMBL4277837 | — | — | 1 | 6.11 |
| CHEMBL4292966 | — | — | 1 | 6.02 |
| CHEMBL4278913 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4285846 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL67 | COMBRETASTATIN A4 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4285810 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4293724 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4290690 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4287325 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4283697 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4290051 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4285231 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4280283 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4289671 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4284722 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4292908 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4282802 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4277874 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4276677 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4286254 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4289588 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4290325 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4289248 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4277924 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4286914 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4278308 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL4285297 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL4281794 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL4285778 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4277837 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL4292966 | — | IC50 | = | 958.0 | nM | 6.02 |
| CHEMBL4278913 | — | IC50 | = | 1018.0 | nM | 5.99 |
| CHEMBL4278193 | — | IC50 | = | 1082.0 | nM | 5.97 |
| CHEMBL4285797 | — | IC50 | = | 1368.0 | nM | 5.86 |
| CHEMBL4289623 | — | IC50 | = | 1791.0 | nM | 5.75 |
| CHEMBL4294093 | — | IC50 | = | 1956.0 | nM | 5.71 |
| CHEMBL4278952 | — | IC50 | = | 2323.0 | nM | 5.63 |
| CHEMBL4287277 | — | IC50 | = | 2648.0 | nM | 5.58 |
| CHEMBL4278990 | — | IC50 | = | 3165.0 | nM | 5.50 |
| CHEMBL4279350 | — | IC50 | = | 4466.0 | nM | 5.35 |
| CHEMBL4290466 | — | IC50 | = | 5137.0 | nM | 5.29 |
| CHEMBL4282374 | — | IC50 | = | 5623.0 | nM | 5.25 |
| CHEMBL4288191 | — | IC50 | = | 6643.0 | nM | 5.18 |
| CHEMBL4282446 | — | IC50 | = | 12845.0 | nM | 4.89 |
| CHEMBL4282770 | — | IC50 | = | 15930.0 | nM | 4.80 |
| CHEMBL4282421 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4288576 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4294840 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4278336 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4286191 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4289172 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4290659 | — | IC50 | > | 20000.0 | nM | - |