Assay Detail
Binding
CHEMBL815873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of tubulin polymerization.
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to the colchicine binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.36 | 6.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1627442 | — | — | 1 | 6.04 |
| CHEMBL1627439 | — | — | 2 | 5.96 |
| CHEMBL1628145 | — | — | 1 | 5.62 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | 2.0 | 1 | 5.54 |
| CHEMBL1627445 | — | — | 1 | 5.52 |
| CHEMBL1627438 | — | — | 1 | 5.38 |
| CHEMBL265926 | — | — | 1 | 5.32 |
| CHEMBL1627441 | — | — | 1 | 5.32 |
| CHEMBL389126 | — | — | 1 | 5.31 |
| CHEMBL1627838 | — | — | 1 | 5.07 |
| CHEMBL1627436 | — | — | 1 | 5.03 |
| CHEMBL189905 | — | — | 1 | 5.00 |
| CHEMBL241993 | — | — | 1 | 4.77 |
| CHEMBL1627843 | — | — | 1 | - |
| CHEMBL242428 | — | — | 1 | - |
| CHEMBL1627434 | — | — | 1 | - |
| CHEMBL1627446 | — | — | 1 | - |
| CHEMBL1627443 | — | — | 1 | - |
| CHEMBL1627440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1627442 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1627439 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1628145 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1627445 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1627438 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL265926 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1627441 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL389126 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1627439 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1627838 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1627436 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL189905 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL241993 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1627440 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL242428 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1627843 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1627434 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1627446 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1627443 | — | IC50 | > | 40000.0 | nM | - |