Assay Detail
Binding
CHEMBL2073498
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Inhibition of KDR by HTRF analysis in presence of 1 mM ATP
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.36 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2071271 | — | — | 1 | 9.00 |
| CHEMBL1980297 | ILORASERTIB | 2.0 | 1 | 8.70 |
| CHEMBL2071276 | — | — | 1 | 8.70 |
| CHEMBL2071275 | — | — | 1 | 8.70 |
| CHEMBL2071216 | — | — | 1 | 8.52 |
| CHEMBL2071273 | — | — | 1 | 8.22 |
| CHEMBL2071270 | — | — | 1 | 8.22 |
| CHEMBL2071217 | — | — | 1 | 8.15 |
| CHEMBL2071274 | — | — | 1 | 8.05 |
| CHEMBL2071200 | — | — | 1 | 7.92 |
| CHEMBL2071201 | — | — | 1 | 7.89 |
| CHEMBL2071202 | — | — | 1 | 7.85 |
| CHEMBL2071277 | — | — | 1 | 7.82 |
| CHEMBL2071272 | — | — | 1 | 7.75 |
| CHEMBL2071211 | — | — | 1 | 7.72 |
| CHEMBL2071210 | — | — | 1 | 7.72 |
| CHEMBL2071199 | — | — | 1 | 7.30 |
| CHEMBL2071206 | — | — | 1 | 7.17 |
| CHEMBL2071203 | — | — | 1 | 7.13 |
| CHEMBL1614709 | — | — | 1 | 7.02 |
| CHEMBL2071215 | — | — | 1 | 6.82 |
| CHEMBL2071213 | — | — | 1 | 6.77 |
| CHEMBL2071214 | — | — | 1 | 6.61 |
| CHEMBL2071208 | — | — | 1 | 6.58 |
| CHEMBL2071205 | — | — | 1 | 6.58 |
| CHEMBL2071207 | — | — | 1 | 6.54 |
| CHEMBL2071194 | — | — | 1 | 6.48 |
| CHEMBL2071209 | — | — | 1 | 6.37 |
| CHEMBL2071196 | — | — | 1 | 6.33 |
| CHEMBL2071212 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2071271 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1980297 | ILORASERTIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2071275 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2071276 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2071216 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2071273 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2071270 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2071217 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2071274 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2071200 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2071201 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2071202 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2071277 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2071272 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2071210 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2071211 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2071199 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2071206 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2071203 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1614709 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2071215 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL2071213 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL2071214 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL2071208 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL2071205 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL2071207 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL2071194 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL2071209 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL2071196 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL2071212 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL2071204 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL2071197 | — | IC50 | = | 922.0 | nM | 6.04 |
| CHEMBL2071198 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL2071195 | — | IC50 | > | 12000.0 | nM | - |