Assay Detail
Binding
CHEMBL4202196
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF-1alpha in human HRE-A549 cells pre-incubated for 1 hr before exposure to hypoxia for 24 hrs by HRE-luciferase reporter gene assay
41
Total Activities
41
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
Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 5.60 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209785 | — | — | 1 | 7.00 |
| CHEMBL4214693 | — | — | 1 | 6.44 |
| CHEMBL4215206 | — | — | 1 | 6.22 |
| CHEMBL4206967 | — | — | 1 | 6.10 |
| CHEMBL4211498 | — | — | 1 | 6.09 |
| CHEMBL4218467 | — | — | 1 | 6.06 |
| CHEMBL4210297 | — | — | 1 | 6.03 |
| CHEMBL4205404 | — | — | 1 | 5.99 |
| CHEMBL4206755 | — | — | 1 | 5.90 |
| CHEMBL4216261 | — | — | 1 | 5.88 |
| CHEMBL2181277 | — | — | 1 | 5.87 |
| CHEMBL4210695 | — | — | 1 | 5.84 |
| CHEMBL4218959 | — | — | 1 | 5.84 |
| CHEMBL4212667 | — | — | 1 | 5.73 |
| CHEMBL4214799 | — | — | 1 | 5.69 |
| CHEMBL4218636 | — | — | 1 | 5.69 |
| CHEMBL2177146 | — | — | 1 | 5.67 |
| CHEMBL4202536 | — | — | 1 | 5.59 |
| CHEMBL4212009 | — | — | 1 | 5.58 |
| CHEMBL4212353 | — | — | 1 | 5.55 |
| CHEMBL4209652 | — | — | 1 | 5.54 |
| CHEMBL4218093 | — | — | 1 | 5.52 |
| CHEMBL4213708 | — | — | 1 | 5.50 |
| CHEMBL4204784 | — | — | 1 | 5.49 |
| CHEMBL4213537 | — | — | 1 | 5.47 |
| CHEMBL4215663 | — | — | 1 | 5.28 |
| CHEMBL4214222 | — | — | 1 | 5.28 |
| CHEMBL4215277 | — | — | 1 | 5.21 |
| CHEMBL4218167 | — | — | 1 | 5.20 |
| CHEMBL4202804 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209785 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4214693 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4215206 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4206967 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4211498 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4218467 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4210297 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4205404 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4206755 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4216261 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL2181277 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL4210695 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL4218959 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4212667 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4218636 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4214799 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL2177146 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL4202536 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL4212009 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL4212353 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL4209652 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL4218093 | — | IC50 | = | 3040.0 | nM | 5.52 |
| CHEMBL4213708 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4204784 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL4213537 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL4215663 | — | IC50 | = | 5280.0 | nM | 5.28 |
| CHEMBL4214222 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL4215277 | — | IC50 | = | 6210.0 | nM | 5.21 |
| CHEMBL4218167 | — | IC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL4202804 | — | IC50 | = | 6520.0 | nM | 5.19 |
| CHEMBL4208298 | — | IC50 | = | 6850.0 | nM | 5.16 |
| CHEMBL4203146 | — | IC50 | = | 7350.0 | nM | 5.13 |
| CHEMBL4210709 | — | IC50 | = | 8450.0 | nM | 5.07 |
| CHEMBL4215953 | — | IC50 | = | 8740.0 | nM | 5.06 |
| CHEMBL4206380 | — | IC50 | = | 8880.0 | nM | 5.05 |
| CHEMBL4209306 | — | IC50 | = | 10780.0 | nM | 4.97 |
| CHEMBL4215392 | — | IC50 | = | 11680.0 | nM | 4.93 |
| CHEMBL4215664 | — | IC50 | = | 12030.0 | nM | 4.92 |
| CHEMBL4217535 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4216129 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL4213782 | — | IC50 | > | 15000.0 | nM | - |