Assay Detail
Binding
CHEMBL5738392
Review assay metadata, readout intent, target linkage, and publication context from the same page.
VEGF ELISA Assay: HEK293 cells are seeded in 96-well poly-lysine coated plates at 20,000 ceils per well in DMEM (10% FBS, 1% NEAA, 0.1% glutamine). Following overnight incubation, the cells are washed with 100 uL of Opti-MEM (Gibco, Carlsbad, Calif.) to remove serum. Compound in DMSO is serially diluted (beginning with 100 μM) in Qpti-MEM and added to the cells. The conditioned media is analyzed for VEGF with a Quantikine human VEGF immunoassay kit (R&D Systems, Minneapolis, Minn.). Optical density measurements at 450 nm are recorded using the Spectra Max 250 (Molecular Devices, Sunnyvale, Calif.). Data defined as % of DFO stimulation is used to calculate EC50 values with GraphPad Prism 4 software (San Diego, Calif.).
63
Total Activities
21
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 receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Prolyl hydroxylase inhibitors and methods of use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 5.05 | 5.85 |
| kon | 21 | - | - |
| k_off | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3646227 | — | — | 3 | 5.85 |
| CHEMBL3646226 | — | — | 3 | 5.48 |
| CHEMBL5926378 | — | — | 3 | 5.37 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 3 | 5.12 |
| CHEMBL3646218 | — | — | 3 | 5.11 |
| CHEMBL3646217 | — | — | 3 | 5.09 |
| CHEMBL3646212 | — | — | 3 | 5.00 |
| CHEMBL3646223 | — | — | 3 | 4.82 |
| CHEMBL3646215 | — | — | 3 | 4.38 |
| CHEMBL3646231 | — | — | 3 | 4.30 |
| CHEMBL3646213 | — | — | 3 | - |
| CHEMBL5787836 | — | — | 3 | - |
| CHEMBL3646216 | — | — | 3 | - |
| CHEMBL3646225 | — | — | 3 | - |
| CHEMBL5876561 | — | — | 3 | - |
| CHEMBL3646229 | — | — | 3 | - |
| CHEMBL5897931 | — | — | 3 | - |
| CHEMBL3646232 | — | — | 3 | - |
| CHEMBL3646233 | — | — | 3 | - |
| CHEMBL3646234 | — | — | 3 | - |
| CHEMBL3646224 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3646227 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3646226 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL5926378 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3646221 | VADADUSTAT | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3646218 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3646217 | — | EC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL3646212 | — | EC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL3646223 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3646215 | — | EC50 | = | 42100.0 | nM | 4.38 |
| CHEMBL3646231 | — | EC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL3646213 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646212 | — | k_off | = | - | s-1 | - |
| CHEMBL3646212 | — | kon | = | - | — | - |
| CHEMBL3646217 | — | kon | = | - | — | - |
| CHEMBL3646234 | — | k_off | = | - | s-1 | - |
| CHEMBL3646234 | — | kon | = | - | — | - |
| CHEMBL3646234 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646233 | — | k_off | = | - | s-1 | - |
| CHEMBL3646225 | — | k_off | = | - | s-1 | - |
| CHEMBL3646233 | — | kon | = | - | — | - |
| CHEMBL3646213 | — | kon | = | - | — | - |
| CHEMBL3646213 | — | k_off | = | - | s-1 | - |
| CHEMBL5787836 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5787836 | — | kon | = | - | — | - |
| CHEMBL5787836 | — | k_off | = | - | s-1 | - |
| CHEMBL3646215 | — | kon | = | - | — | - |
| CHEMBL3646215 | — | k_off | = | - | s-1 | - |
| CHEMBL3646216 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646216 | — | kon | = | - | — | - |
| CHEMBL3646216 | — | k_off | = | - | s-1 | - |
| CHEMBL3646226 | — | kon | = | - | — | - |
| CHEMBL3646229 | — | kon | = | - | — | - |
| CHEMBL5897931 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646229 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5876561 | — | k_off | = | - | s-1 | - |
| CHEMBL5876561 | — | kon | = | - | — | - |
| CHEMBL5876561 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646227 | — | k_off | = | - | s-1 | - |
| CHEMBL3646227 | — | kon | = | - | — | - |
| CHEMBL3646226 | — | k_off | = | - | s-1 | - |
| CHEMBL3646233 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646229 | — | k_off | = | - | s-1 | - |
| CHEMBL3646224 | — | kon | = | - | — | - |
| CHEMBL5897931 | — | kon | = | - | — | - |
| CHEMBL5897931 | — | k_off | = | - | s-1 | - |
| CHEMBL3646231 | — | kon | = | - | — | - |
| CHEMBL3646231 | — | k_off | = | - | s-1 | - |
| CHEMBL3646232 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3646232 | — | kon | = | - | — | - |
| CHEMBL3646232 | — | k_off | = | - | s-1 | - |