Assay Detail
Binding
CHEMBL1292980
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Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay
25
Total Activities
25
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
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.27 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 9.80 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 9.60 |
| CHEMBL1289925 | — | — | 1 | 9.47 |
| CHEMBL1290030 | — | — | 1 | 8.80 |
| CHEMBL1290362 | — | — | 1 | 8.54 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 8.52 |
| CHEMBL1290136 | — | — | 1 | 8.47 |
| CHEMBL333021 | L-21649 | 1.0 | 1 | 8.40 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 8.40 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 8.40 |
| CHEMBL1290137 | — | — | 1 | 8.39 |
| CHEMBL1290031 | — | — | 1 | 8.39 |
| CHEMBL1290471 | — | — | 1 | 8.38 |
| CHEMBL1290247 | ASN01107570 | — | 1 | 8.30 |
| CHEMBL1290470 | — | — | 1 | 8.25 |
| CHEMBL1290246 | — | — | 1 | 8.23 |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | 8.22 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.05 |
| CHEMBL1290361 | ASN06356088 | — | 1 | 8.00 |
| CHEMBL153843 | — | — | 1 | 7.64 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.52 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 7.43 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.40 |
| CHEMBL1289705 | — | — | 1 | 7.11 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289494 | TIVOZANIB | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL1289926 | AXITINIB | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL1289925 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL1290030 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1290362 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL572881 | MOTESANIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1290136 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL333021 | L-21649 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL491473 | CEDIRANIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1289601 | LENVATINIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1290137 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1290031 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1290471 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1290247 | ASN01107570 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1290470 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1290246 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL2079588 | TELATINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL535 | SUNITINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1290361 | ASN06356088 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL153843 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL477772 | PAZOPANIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL101253 | VATALANIB | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1289705 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 90.0 | nM | 7.05 |