Assay Detail
Binding
CHEMBL931441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | AGS |
| 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
Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.71 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | 2.0 | 1 | 8.44 |
| CHEMBL408851 | ACETYLBAKUCHIOL | — | 1 | 5.24 |
| CHEMBL262344 | BAKUCHIOL | 1.0 | 1 | 5.21 |
| CHEMBL262630 | — | — | 1 | 5.06 |
| CHEMBL260776 | — | — | 1 | 4.58 |
| CHEMBL261315 | — | — | 1 | - |
| CHEMBL405046 | — | — | 1 | - |
| CHEMBL258478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL408851 | ACETYLBAKUCHIOL | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL262344 | BAKUCHIOL | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL262630 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL260776 | — | IC50 | = | 26300.0 | nM | 4.58 |
| CHEMBL261315 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL405046 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL258478 | — | IC50 | > | 50000.0 | nM | - |