Assay Detail
Binding
CHEMBL3380585
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF1 signaling in human U251 cells expressing VEGF by VEGF promoter-driven PLAP reporter gene assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| 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
Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.09 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3335630 | — | — | 1 | 9.33 |
| CHEMBL3335423 | — | — | 1 | 9.01 |
| CHEMBL3335427 | — | — | 1 | 8.96 |
| CHEMBL3335426 | — | — | 1 | 8.59 |
| CHEMBL3335421 | — | — | 1 | 8.51 |
| CHEMBL3335415 | — | — | 1 | 8.48 |
| CHEMBL3335425 | — | — | 1 | 8.24 |
| CHEMBL3335411 | — | — | 1 | 8.10 |
| CHEMBL3335419 | — | — | 1 | 8.10 |
| CHEMBL3335416 | — | — | 1 | 7.89 |
| CHEMBL3335410 | — | — | 1 | 7.89 |
| CHEMBL3335413 | — | — | 1 | 7.85 |
| CHEMBL3335424 | — | — | 1 | 7.68 |
| CHEMBL3335417 | — | — | 1 | 7.52 |
| CHEMBL3335420 | — | — | 1 | 7.47 |
| CHEMBL3335418 | — | — | 1 | 7.46 |
| CHEMBL3335412 | — | — | 1 | 6.96 |
| CHEMBL3335414 | — | — | 1 | 6.92 |
| CHEMBL3335403 | — | — | 1 | 6.64 |
| CHEMBL3335135 | — | — | 1 | 6.55 |
| CHEMBL3335134 | — | — | 1 | 6.25 |
| CHEMBL3335406 | — | — | 1 | 6.06 |
| CHEMBL3335405 | — | — | 1 | 5.80 |
| CHEMBL3335408 | — | — | 1 | 5.66 |
| CHEMBL3335136 | — | — | 1 | 5.66 |
| CHEMBL3335407 | — | — | 1 | 5.60 |
| CHEMBL3335409 | — | — | 1 | 5.60 |
| CHEMBL3335139 | — | — | 1 | 5.40 |
| CHEMBL3335404 | — | — | 1 | 5.35 |
| CHEMBL3335137 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3335630 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL3335423 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL3335427 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3335426 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3335421 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3335415 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3335425 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3335411 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3335419 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3335416 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3335410 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3335413 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3335424 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3335417 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3335420 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3335418 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3335412 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3335414 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3335403 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3335135 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3335134 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3335406 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3335405 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3335408 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3335136 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3335409 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3335407 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3335139 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3335404 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3335137 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3335133 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL3335402 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3335401 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3335422 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL3335138 | — | IC50 | > | 20000.0 | nM | - |