Assay Detail
Binding
CHEMBL1034023
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Inhibition of VEGFR1 assessed as blockade of pGAT-biotin phosphorylation in presence of 2 uM ATP by HTRF assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.38 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473287 | — | — | 1 | 7.26 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.85 |
| CHEMBL153843 | — | — | 1 | 6.77 |
| CHEMBL515880 | — | — | 1 | 6.77 |
| CHEMBL470441 | — | — | 1 | 6.72 |
| CHEMBL475704 | — | — | 1 | 6.60 |
| CHEMBL475709 | — | — | 1 | 6.60 |
| CHEMBL475509 | — | — | 1 | 6.58 |
| CHEMBL473288 | — | — | 1 | 6.58 |
| CHEMBL475510 | — | — | 1 | 6.51 |
| CHEMBL517399 | — | — | 1 | 6.48 |
| CHEMBL474709 | — | — | 1 | 6.42 |
| CHEMBL458531 | — | — | 1 | 6.24 |
| CHEMBL475708 | — | — | 1 | 6.21 |
| CHEMBL512863 | — | — | 1 | 6.17 |
| CHEMBL462315 | — | — | 1 | 6.16 |
| CHEMBL470440 | — | — | 1 | 6.12 |
| CHEMBL473268 | — | — | 1 | 6.01 |
| CHEMBL443921 | — | — | 1 | 5.96 |
| CHEMBL516243 | — | — | 1 | 5.91 |
| CHEMBL512862 | — | — | 1 | 5.75 |
| CHEMBL460191 | — | — | 1 | 5.60 |
| CHEMBL474494 | — | — | 1 | - |
| CHEMBL474293 | — | — | 1 | - |
| CHEMBL518204 | — | — | 1 | - |
| CHEMBL462527 | — | — | 1 | - |
| CHEMBL462528 | — | — | 1 | - |
| CHEMBL475703 | — | — | 1 | - |
| CHEMBL514986 | — | — | 1 | - |
| CHEMBL512380 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473287 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL101253 | VATALANIB | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL153843 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL515880 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL470441 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL475704 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL475709 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL475509 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL473288 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL475510 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL517399 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL474709 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL458531 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL475708 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL512863 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL462315 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL470440 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL473268 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL443921 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL516243 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL512862 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL460191 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL474494 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL474293 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL518204 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL462527 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL462528 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL475703 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL514986 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL512380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL458532 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL509737 | — | IC50 | > | 10000.0 | nM | - |