Assay Detail
Binding
CHEMBL4356100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF1alpha transcriptional activity in hypoxia-induced human HCCLM3 cells co-transfected with luciferase reporter plasmid containing five copies of HREs and pRL-SV40 plasmid encoding Renilla luciferase incubated with compound under normoxia for 1 hr followed by hypoxia induction and measured after 24 hrs by HRE-dependent dual luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.33 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447149 | — | — | 1 | 6.50 |
| CHEMBL4556236 | — | — | 1 | 6.03 |
| CHEMBL4474416 | — | — | 1 | 5.85 |
| CHEMBL4582907 | — | — | 1 | 5.67 |
| CHEMBL4524481 | — | — | 1 | 5.61 |
| CHEMBL4463336 | — | — | 1 | 5.54 |
| CHEMBL427092 | — | — | 1 | 5.51 |
| CHEMBL4471787 | — | — | 1 | 5.37 |
| CHEMBL4436783 | — | — | 1 | 5.34 |
| CHEMBL4585779 | — | — | 1 | 5.13 |
| CHEMBL4538482 | — | — | 1 | 5.07 |
| CHEMBL4532373 | — | — | 1 | 5.01 |
| CHEMBL4532078 | — | — | 1 | 5.01 |
| CHEMBL4514880 | — | — | 1 | 5.00 |
| CHEMBL4459452 | — | — | 1 | 4.93 |
| CHEMBL4517735 | — | — | 1 | 4.86 |
| CHEMBL4437373 | — | — | 1 | 4.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447149 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4556236 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4474416 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4582907 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL4524481 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL4463336 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL427092 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL4471787 | — | IC50 | = | 4240.0 | nM | 5.37 |
| CHEMBL4436783 | — | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL4585779 | — | IC50 | = | 7320.0 | nM | 5.13 |
| CHEMBL4538482 | — | IC50 | = | 8530.0 | nM | 5.07 |
| CHEMBL4532373 | — | IC50 | = | 9840.0 | nM | 5.01 |
| CHEMBL4532078 | — | IC50 | = | 9840.0 | nM | 5.01 |
| CHEMBL4514880 | — | IC50 | = | 10040.0 | nM | 5.00 |
| CHEMBL4459452 | — | IC50 | = | 11610.0 | nM | 4.93 |
| CHEMBL4517735 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL4437373 | — | IC50 | = | 55700.0 | nM | 4.25 |