Assay Detail
Binding
CHEMBL1695274
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR-2 kinase assessed as phosphorylated level of pGAT-biotin peptide preincubated for 5 to 10 mins before addition of substrate measured after 2 hrs by HTRF assay
28
Total Activities
28
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
Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.89 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1688357 | — | — | 1 | 6.82 |
| CHEMBL1688350 | — | — | 1 | 6.80 |
| CHEMBL204754 | — | — | 1 | 6.77 |
| CHEMBL1087218 | — | — | 1 | 6.68 |
| CHEMBL1688352 | — | — | 1 | 6.52 |
| CHEMBL1087349 | — | — | 1 | 6.08 |
| CHEMBL1688246 | — | — | 1 | 5.96 |
| CHEMBL1688351 | — | — | 1 | 5.85 |
| CHEMBL204710 | — | — | 1 | 5.72 |
| CHEMBL1688249 | — | — | 1 | 5.64 |
| CHEMBL1688248 | — | — | 1 | 5.60 |
| CHEMBL203642 | — | — | 1 | 5.58 |
| CHEMBL1688356 | — | — | 1 | 5.51 |
| CHEMBL1688354 | — | — | 1 | 5.50 |
| CHEMBL1688344 | — | — | 1 | 5.50 |
| CHEMBL1688346 | — | — | 1 | 5.47 |
| CHEMBL1688250 | — | — | 1 | 5.35 |
| CHEMBL1688355 | — | — | 1 | 5.34 |
| CHEMBL1688353 | — | — | 1 | 5.29 |
| CHEMBL203062 | — | — | 1 | - |
| CHEMBL1688349 | — | — | 1 | - |
| CHEMBL1688348 | — | — | 1 | - |
| CHEMBL205166 | — | — | 1 | - |
| CHEMBL1688347 | — | — | 1 | - |
| CHEMBL1688345 | — | — | 1 | - |
| CHEMBL381122 | — | — | 1 | - |
| CHEMBL382359 | — | — | 1 | - |
| CHEMBL1688247 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1688357 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1688350 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL204754 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1087218 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1688352 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1087349 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1688246 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1688351 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL204710 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL1688249 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1688248 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL203642 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1688356 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1688354 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1688344 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL1688346 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL1688250 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1688355 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1688353 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL203062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688349 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688348 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688347 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688345 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL381122 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL382359 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1688247 | — | IC50 | > | 10000.0 | nM | - |