Assay Detail
Binding
CHEMBL4401535
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human (His8)2-tagged fascin (1 to 493 residues) expressed in Escherichia coli BL21(DE3) pLysS assessed as reduction in F-actin bundling preincubated for 30 mins followed by F-actin addition and measured after 45 mins by Coomassie blue staining-based SDS-PAGE analysis
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.52 | 6.62 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452711 | — | — | 1 | 6.62 |
| CHEMBL4461540 | — | — | 1 | 6.48 |
| CHEMBL4574198 | — | — | 1 | 6.29 |
| CHEMBL4566108 | — | — | 1 | 6.20 |
| CHEMBL4559691 | — | — | 1 | 6.20 |
| CHEMBL4451624 | — | — | 1 | 5.89 |
| CHEMBL4457641 | — | — | 1 | 5.68 |
| CHEMBL4516481 | — | — | 1 | 5.42 |
| CHEMBL4544795 | — | — | 1 | 5.34 |
| CHEMBL4584583 | — | — | 1 | 5.28 |
| CHEMBL4527032 | — | — | 1 | 5.07 |
| CHEMBL4455723 | — | — | 1 | 4.98 |
| CHEMBL4543704 | — | — | 1 | 4.94 |
| CHEMBL4469510 | — | — | 1 | 4.17 |
| CHEMBL4440859 | — | — | 1 | 4.17 |
| CHEMBL4439645 | — | — | 1 | - |
| CHEMBL4564438 | — | — | 1 | - |
| CHEMBL4574928 | — | — | 1 | - |
| CHEMBL4537924 | — | — | 1 | - |
| CHEMBL4462533 | — | — | 1 | - |
| CHEMBL4472315 | — | — | 1 | - |
| CHEMBL4574047 | — | — | 1 | - |
| CHEMBL4448440 | — | — | 1 | - |
| CHEMBL4592515 | — | — | 1 | - |
| CHEMBL4576435 | — | — | 1 | - |
| CHEMBL4470509 | — | — | 1 | - |
| CHEMBL4539975 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452711 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4461540 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4574198 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4566108 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4559691 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4451624 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4457641 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4516481 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4544795 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4584583 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4527032 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4455723 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4543704 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4469510 | — | IC50 | = | 67900.0 | nM | 4.17 |
| CHEMBL4440859 | — | IC50 | = | 67600.0 | nM | 4.17 |
| CHEMBL4439645 | — | IC50 | - | — | - | |
| CHEMBL4564438 | — | IC50 | - | — | - | |
| CHEMBL4574928 | — | IC50 | - | — | - | |
| CHEMBL4537924 | — | IC50 | - | — | - | |
| CHEMBL4462533 | — | IC50 | - | — | - | |
| CHEMBL4472315 | — | IC50 | - | — | - | |
| CHEMBL4574047 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4448440 | — | IC50 | - | — | - | |
| CHEMBL4592515 | — | Inhibition | - | % | - | |
| CHEMBL4576435 | — | IC50 | - | — | - | |
| CHEMBL4470509 | — | IC50 | - | — | - | |
| CHEMBL4539975 | — | IC50 | - | — | - |