Assay Detail
Binding
CHEMBL5733319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ELISA Assay: Four hours later, serial dilutions of 10× compound stocks were made in growth medium from 500×DMSO stocks, and 20 μL of those 10× stocks were added to each well to make final concentrations as follows (μM): 20, 6.67, 2.22, 0.74, 0.25, 0.082, 0.027, 0.009, 0.003, 0.001, and 0. Each concentration had duplicated wells. About 20 hours later, medium was removed by suction and each well was supplied with 180 μL of growth medium. About 20 μl freshly-made 10× compound stocks were added to each well. About 24 hours later, cell culture medium was removed for the determination of VEGFA concentration using an ELISA kit purchased from R&D systems by following the manufacturer's suggested method. The EC50 was calculated by GraphPad Prism using the dose-response-inhibition (four parameter) equation. The cell seeded plate was then subjected to CellTiter-Glo luminescence cell viability assay (Promega) by adding 50 μL of Celltiter Glo reagent into each well and shaking the plate for 8 minutes at 550 rpm (Thermomixer R, Eppendorf) then read luminescence signal in plate reader (3 second delay, 0.5 second/well integration time, Synergy 2 multi Detection Microplate reader) immediately.
204
Total Activities
65
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor A, long form (CHEMBL1783) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aryl ethers and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 68 | 7.16 | 9.00 |
| kon | 68 | - | - |
| k_off | 68 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5848806 | — | — | 3 | 9.00 |
| CHEMBL4176457 | — | — | 3 | 8.40 |
| CHEMBL5801572 | — | — | 3 | 8.22 |
| CHEMBL5986684 | — | — | 3 | 8.22 |
| CHEMBL4453227 | — | — | 3 | 8.21 |
| CHEMBL5951034 | — | — | 3 | 8.21 |
| CHEMBL6025188 | — | — | 3 | 8.15 |
| CHEMBL5794926 | — | — | 3 | 7.96 |
| CHEMBL5778334 | — | — | 3 | 7.89 |
| CHEMBL4165848 | — | — | 3 | 7.89 |
| CHEMBL6009433 | — | — | 6 | 7.85 |
| CHEMBL4161350 | — | — | 3 | 7.82 |
| CHEMBL5920970 | — | — | 3 | 7.82 |
| CHEMBL5849506 | — | — | 3 | 7.80 |
| CHEMBL4585668 | BELZUTIFAN | 4.0 | 3 | 7.75 |
| CHEMBL6055730 | — | — | 6 | 7.72 |
| CHEMBL4162398 | — | — | 3 | 7.70 |
| CHEMBL5853706 | — | — | 3 | 7.58 |
| CHEMBL5957443 | — | — | 3 | 7.55 |
| CHEMBL5933231 | — | — | 3 | 7.55 |
| CHEMBL5948559 | — | — | 3 | 7.54 |
| CHEMBL4169277 | — | — | 3 | 7.48 |
| CHEMBL6007916 | — | — | 3 | 7.46 |
| CHEMBL4167415 | — | — | 3 | 7.43 |
| CHEMBL5970241 | — | — | 3 | 7.42 |
| CHEMBL5963912 | — | — | 3 | 7.40 |
| CHEMBL4173075 | — | — | 3 | 7.38 |
| CHEMBL5983818 | — | — | 3 | 7.33 |
| CHEMBL6022087 | — | — | 3 | 7.32 |
| CHEMBL5868442 | — | — | 3 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5848806 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4176457 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5986684 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5801572 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4453227 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5951034 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL6025188 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5794926 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4165848 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5778334 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL6009433 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5920970 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4161350 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5849506 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6009433 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4585668 | BELZUTIFAN | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL6055730 | — | EC50 | = | 19.2 | nM | 7.72 |
| CHEMBL6055730 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4162398 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5853706 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5957443 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5933231 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5948559 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4169277 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL6007916 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4167415 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5970241 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5963912 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4173075 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5983818 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL6022087 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5868442 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5960698 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5993390 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL6060195 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5776788 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5886427 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4169671 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5828252 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL6053931 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5940475 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5980618 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5859559 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5846164 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5785748 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5964876 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5885510 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5940475 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4160209 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5761841 | — | EC50 | = | 180.0 | nM | 6.75 |