Assay Detail
Binding
CHEMBL932926
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Inhibition of VEGFR2
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.31 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250625 | — | — | 1 | 8.77 |
| CHEMBL400402 | — | — | 1 | 8.66 |
| CHEMBL250213 | — | — | 1 | 8.57 |
| CHEMBL249821 | — | — | 1 | 8.33 |
| CHEMBL230686 | — | — | 1 | 6.89 |
| CHEMBL230685 | — | — | 1 | 6.28 |
| CHEMBL250214 | — | — | 1 | 6.28 |
| CHEMBL436137 | — | — | 1 | 6.25 |
| CHEMBL268825 | — | — | 1 | 5.72 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250625 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL400402 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL250213 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL249821 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL230686 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL230685 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL250214 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL436137 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL268825 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL403989 | TG100-801 | IC50 | >= | 10000.0 | nM | - |