Assay Detail
Binding
CHEMBL4122817
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF-1alpha/p300/CBP (unknown origin) transcriptional activity expressed in human HeLa cells expressing HRE-Luc/CMV-Luc after 12 hrs under hypoxic condition by dual luciferase reporter gene assay
6
Total Activities
6
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 | Intermediate |
Target
HIF1A/p300/CREB-binding protein (CHEMBL4296108) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Discovery of bicyclo[3,3,1]non-2-ene as a novel skeleton for HIF-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.20 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333985 | — | — | 1 | 5.89 |
| CHEMBL4126974 | — | — | 1 | 5.52 |
| CHEMBL4128348 | — | — | 1 | 5.20 |
| CHEMBL4129341 | — | — | 1 | 4.19 |
| CHEMBL4125744 | — | — | 1 | - |
| CHEMBL4127113 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333985 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4126974 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4128348 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4129341 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL4125744 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4127113 | — | IC50 | > | 100000.0 | nM | - |