Assay Detail
Binding
CHEMBL864972
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Inhibition of VEGFR1 phosphorylation in presence of 2 uM ATP by HTRF assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 6.40 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.00 |
| CHEMBL382218 | — | — | 1 | 6.92 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.85 |
| CHEMBL383123 | — | — | 1 | 6.85 |
| CHEMBL202011 | — | — | 1 | 6.80 |
| CHEMBL153843 | — | — | 1 | 6.77 |
| CHEMBL382610 | — | — | 1 | 6.75 |
| CHEMBL204984 | — | — | 1 | 6.66 |
| CHEMBL383334 | — | — | 1 | 6.66 |
| CHEMBL206123 | — | — | 1 | 6.58 |
| CHEMBL207975 | — | — | 1 | 6.57 |
| CHEMBL204621 | — | — | 1 | 6.57 |
| CHEMBL381182 | — | — | 1 | 6.50 |
| CHEMBL206136 | — | — | 1 | 6.36 |
| CHEMBL207772 | — | — | 1 | 6.33 |
| CHEMBL383333 | — | — | 1 | 6.32 |
| CHEMBL205050 | — | — | 1 | 6.30 |
| CHEMBL382142 | — | — | 1 | 6.28 |
| CHEMBL380536 | — | — | 1 | 6.25 |
| CHEMBL377995 | — | — | 1 | 6.21 |
| CHEMBL205244 | — | — | 1 | 6.17 |
| CHEMBL205639 | — | — | 1 | 6.15 |
| CHEMBL205502 | — | — | 1 | 6.14 |
| CHEMBL381293 | — | — | 1 | 6.13 |
| CHEMBL381577 | — | — | 1 | 6.12 |
| CHEMBL205325 | — | — | 1 | 6.11 |
| CHEMBL205544 | — | — | 1 | 6.09 |
| CHEMBL208363 | — | — | 1 | 6.08 |
| CHEMBL383434 | — | — | 1 | 6.03 |
| CHEMBL204425 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24828 | VANDETANIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL382218 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL383123 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL101253 | VATALANIB | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL202011 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL153843 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL382610 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL204984 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL383334 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL206123 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL207975 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL204621 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL381182 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL206136 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL207772 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL383333 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL205050 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL382142 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL380536 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL377995 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL205244 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL205639 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL205502 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL381293 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL381577 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL205325 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL205544 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL208363 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL383434 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL204425 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL205421 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL382797 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205684 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL207099 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL207049 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL207821 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL380421 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205647 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL206670 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL204846 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL381704 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL206089 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL205901 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL208229 | — | IC50 | > | 10000.0 | nM | - |