Assay Detail
Binding
CHEMBL2327238
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Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.18 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323956 | — | — | 1 | 7.85 |
| CHEMBL2323957 | — | — | 1 | 7.47 |
| CHEMBL253429 | — | — | 1 | 6.67 |
| CHEMBL2323955 | — | — | 1 | 6.57 |
| CHEMBL2323952 | — | — | 1 | 5.85 |
| CHEMBL333985 | — | — | 1 | 5.82 |
| CHEMBL2323954 | — | — | 1 | 5.50 |
| CHEMBL2323953 | — | — | 1 | 5.21 |
| CHEMBL427092 | — | — | 1 | 4.68 |
| CHEMBL2323951 | — | — | 1 | - |
| CHEMBL432219 | — | — | 1 | - |
| CHEMBL2323950 | — | — | 1 | - |
| CHEMBL371949 | — | — | 1 | - |
| CHEMBL200726 | — | — | 1 | - |
| CHEMBL371910 | — | — | 1 | - |
| CHEMBL175596 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323956 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2323957 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL253429 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL2323955 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2323952 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL333985 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2323954 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2323953 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL427092 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2323951 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL432219 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2323950 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL371949 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL200726 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL371910 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL175596 | — | IC50 | > | 30000.0 | nM | - |