Assay Detail
Binding
CHEMBL3869978
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Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha (CHEMBL2221345) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.79 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333985 | — | — | 1 | 5.92 |
| CHEMBL3927498 | — | — | 1 | 5.43 |
| CHEMBL3899458 | — | — | 1 | 5.19 |
| CHEMBL3918550 | — | — | 1 | 5.13 |
| CHEMBL3936460 | — | — | 1 | 5.04 |
| CHEMBL3908512 | — | — | 1 | 5.03 |
| CHEMBL3918157 | — | — | 1 | 4.77 |
| CHEMBL3915177 | — | — | 1 | 4.60 |
| CHEMBL3946046 | — | — | 1 | 4.41 |
| CHEMBL3892315 | — | — | 1 | 4.25 |
| CHEMBL3918408 | — | — | 1 | 4.21 |
| CHEMBL3961295 | — | — | 1 | 4.16 |
| CHEMBL3940432 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333985 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3927498 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3899458 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3918550 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3936460 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3908512 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3918157 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3915177 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3946046 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3892315 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL3918408 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL3961295 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL3940432 | — | IC50 | = | 75000.0 | nM | 4.12 |