Assay Detail
Binding
CHEMBL828488
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Inhibitory concentration against human VEGFR2 kinase
27
Total Activities
27
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 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.48 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189354 | — | — | 1 | 9.00 |
| CHEMBL185716 | — | — | 1 | 9.00 |
| CHEMBL188025 | — | — | 1 | 8.70 |
| CHEMBL188381 | GW806742X | — | 1 | 8.70 |
| CHEMBL188997 | — | — | 1 | 8.70 |
| CHEMBL189862 | — | — | 1 | 8.52 |
| CHEMBL187627 | — | — | 1 | 8.40 |
| CHEMBL2096808 | — | — | 1 | 8.30 |
| CHEMBL187609 | — | — | 1 | 8.22 |
| CHEMBL189408 | — | — | 1 | 7.96 |
| CHEMBL425718 | — | — | 1 | 7.77 |
| CHEMBL185695 | — | — | 1 | 7.75 |
| CHEMBL186369 | — | — | 1 | 7.58 |
| CHEMBL188149 | — | — | 1 | 7.54 |
| CHEMBL365866 | — | — | 1 | 7.51 |
| CHEMBL189291 | — | — | 1 | 7.46 |
| CHEMBL189353 | GW809897X | — | 1 | 7.19 |
| CHEMBL187033 | — | — | 1 | 7.02 |
| CHEMBL189199 | — | — | 1 | 6.93 |
| CHEMBL187494 | — | — | 1 | 6.82 |
| CHEMBL189305 | — | — | 1 | 6.75 |
| CHEMBL187361 | — | — | 1 | 6.57 |
| CHEMBL188421 | — | — | 1 | 6.49 |
| CHEMBL188042 | — | — | 1 | 6.17 |
| CHEMBL363316 | — | — | 1 | 6.00 |
| CHEMBL187930 | — | — | 1 | 5.51 |
| CHEMBL364115 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189354 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL185716 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL188025 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL188381 | GW806742X | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL188997 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL189862 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL187627 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2096808 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL187609 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL189408 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL425718 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL185695 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL186369 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL188149 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL365866 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL189291 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL189353 | GW809897X | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL187033 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL189199 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL187494 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL189305 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL187361 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL188421 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL188042 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL363316 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL187930 | — | IC50 | = | 3114.0 | nM | 5.51 |
| CHEMBL364115 | — | IC50 | = | 4490.0 | nM | 5.35 |