Assay Detail
Binding
CHEMBL4614037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF1alpha transcriptional activity in human HeLa cells transfected with HRE-firefly luciferase and cytomegalovirus-promoter expressing Renilla luciferase incubated for 12 hrs under 1% O2 condition by dual luciferase reporter gene assay
10
Total Activities
10
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
Design, synthesis, and evaluation of indeno[2,1-c]pyrazolones for use as inhibitors against hypoxia-inducible factor (HIF)-1 transcriptional activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.58 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643958 | — | — | 1 | 6.41 |
| CHEMBL4645257 | — | — | 1 | 6.21 |
| CHEMBL4635527 | — | — | 1 | 6.10 |
| CHEMBL4648415 | — | — | 1 | 5.85 |
| CHEMBL333985 | — | — | 1 | 5.62 |
| CHEMBL4633187 | — | — | 1 | 5.32 |
| CHEMBL4640990 | — | — | 1 | 5.06 |
| CHEMBL4635362 | — | — | 1 | 5.00 |
| CHEMBL4646675 | — | — | 1 | 4.64 |
| CHEMBL4638844 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643958 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4645257 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4635527 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4648415 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL333985 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4633187 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4640990 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4635362 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4646675 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4638844 | — | IC50 | > | 30000.0 | nM | - |