Assay Detail
Binding
CHEMBL4403233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal His10-tagged LOXL2 (Met1 to Gln774 residues) expressed in mouse NS0 cells using cadaverine hydrochloride as substrate preincubated for 3 hrs followed by substrate addition by ROS-Glo assay
11
Total Activities
11
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
2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.74 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4568508 | — | — | 1 | 7.16 |
| CHEMBL4457897 | — | — | 1 | 7.16 |
| CHEMBL4444163 | — | — | 1 | 7.11 |
| CHEMBL4550042 | — | — | 1 | 7.07 |
| CHEMBL4457629 | — | — | 1 | 6.92 |
| CHEMBL4441173 | — | — | 1 | 6.90 |
| CHEMBL4574361 | — | — | 1 | 6.84 |
| CHEMBL4463882 | — | — | 1 | 6.75 |
| CHEMBL1618272 | — | — | 1 | 6.43 |
| CHEMBL4443558 | — | — | 1 | 6.33 |
| CHEMBL4565942 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4568508 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4457897 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4444163 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4550042 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4457629 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4441173 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4574361 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4463882 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL1618272 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4443558 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4565942 | — | IC50 | = | 3190.0 | nM | 5.50 |