Assay Detail
Binding
CHEMBL5225194
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Inhibition of Heparanase-1 (unknown origin) by HTRF method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead identification of novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent heparanase-1 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.89 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5273557 | — | — | 1 | 5.47 |
| CHEMBL5284745 | — | — | 1 | 5.39 |
| CHEMBL5276305 | — | — | 1 | 5.10 |
| CHEMBL5280906 | — | — | 1 | 5.09 |
| CHEMBL3347523 | — | — | 1 | 5.04 |
| CHEMBL5280810 | — | — | 1 | 4.95 |
| CHEMBL5290753 | — | — | 1 | 4.92 |
| CHEMBL5281456 | — | — | 1 | 4.72 |
| CHEMBL5273519 | — | — | 1 | 4.71 |
| CHEMBL5279462 | — | — | 1 | 4.71 |
| CHEMBL5283021 | — | — | 1 | 4.67 |
| CHEMBL5270267 | — | — | 1 | 4.52 |
| CHEMBL4650593 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5273557 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL5284745 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL5276305 | — | IC50 | = | 7890.0 | nM | 5.10 |
| CHEMBL5280906 | — | IC50 | = | 8030.0 | nM | 5.09 |
| CHEMBL3347523 | — | IC50 | = | 9190.0 | nM | 5.04 |
| CHEMBL5280810 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL5290753 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5281456 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL5273519 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL5279462 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL5283021 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL5270267 | — | IC50 | = | 30500.0 | nM | 4.52 |
| CHEMBL4650593 | — | IC50 | = | 50100.0 | nM | 4.30 |