Assay Detail
Binding
CHEMBL3374592
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Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.25 | 5.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3359141 | — | — | 1 | 5.37 |
| CHEMBL427092 | — | — | 1 | 5.36 |
| CHEMBL3359147 | — | — | 1 | 5.33 |
| CHEMBL3359145 | — | — | 1 | 4.94 |
| CHEMBL3359142 | — | — | 1 | - |
| CHEMBL3359143 | — | — | 1 | - |
| CHEMBL3359144 | — | — | 1 | - |
| CHEMBL3359146 | — | — | 1 | - |
| CHEMBL3359148 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3359141 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL427092 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3359147 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3359145 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL3359142 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3359143 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3359144 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3359146 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3359148 | — | IC50 | > | 30000.0 | nM | - |