Assay Detail
Binding
CHEMBL5120693
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Inhibition of HIF-1alpha (unknown origin) transcriptional activity expressed in HEK293T cells co-transfected with renilla and HRE-firelfly luciferase incubated for 24 hrs by dual luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzo[<i>d</i>]isoxazole Derivatives as Hypoxia-Inducible Factor (HIF)-1α Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.34 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5205360 | — | — | 1 | 7.62 |
| CHEMBL5184354 | — | — | 1 | 7.62 |
| CHEMBL5208153 | — | — | 1 | 7.40 |
| CHEMBL5194403 | — | — | 1 | 7.39 |
| CHEMBL5197796 | — | — | 1 | 7.38 |
| CHEMBL5192165 | — | — | 1 | 7.12 |
| CHEMBL5188937 | — | — | 1 | 6.77 |
| CHEMBL5174696 | — | — | 1 | 6.70 |
| CHEMBL5202378 | — | — | 1 | 6.60 |
| CHEMBL5178011 | — | — | 1 | 6.51 |
| CHEMBL5177951 | — | — | 1 | 6.32 |
| CHEMBL5209002 | — | — | 1 | 6.19 |
| CHEMBL5190853 | — | — | 1 | 6.19 |
| CHEMBL5205347 | — | — | 1 | 6.09 |
| CHEMBL5189187 | — | — | 1 | 6.03 |
| CHEMBL5186754 | — | — | 1 | 5.77 |
| CHEMBL1078237 | — | — | 1 | 5.64 |
| CHEMBL427092 | — | — | 1 | 5.58 |
| CHEMBL5199345 | — | — | 1 | 5.27 |
| CHEMBL5207932 | — | — | 1 | 5.26 |
| CHEMBL5188651 | — | — | 1 | 5.13 |
| CHEMBL5188998 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5205360 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5184354 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5208153 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5194403 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5197796 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5192165 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5188937 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5174696 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5202378 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5178011 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5177951 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5209002 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5190853 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5205347 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5189187 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5186754 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1078237 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL427092 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5199345 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL5207932 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5188651 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5188998 | — | IC50 | = | 10000.0 | nM | 5.00 |