Assay Detail
Binding
CHEMBL2073500
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Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| 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 | 7.46 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1980297 | ILORASERTIB | 2.0 | 1 | 8.52 |
| CHEMBL2071216 | — | — | 1 | 8.10 |
| CHEMBL2071201 | — | — | 1 | 8.05 |
| CHEMBL1614709 | — | — | 1 | 7.72 |
| CHEMBL2071202 | — | — | 1 | 7.70 |
| CHEMBL2071200 | — | — | 1 | 7.46 |
| CHEMBL2071217 | — | — | 1 | 7.38 |
| CHEMBL2071276 | — | — | 1 | 7.36 |
| CHEMBL2071270 | — | — | 1 | 7.32 |
| CHEMBL2071277 | — | — | 1 | 7.31 |
| CHEMBL2071275 | — | — | 1 | 7.26 |
| CHEMBL2071203 | — | — | 1 | 7.21 |
| CHEMBL2071274 | — | — | 1 | 7.11 |
| CHEMBL2071210 | — | — | 1 | 7.08 |
| CHEMBL2071273 | — | — | 1 | 7.05 |
| CHEMBL2071272 | — | — | 1 | 6.78 |
| CHEMBL2071194 | — | — | 1 | - |
| CHEMBL2071199 | — | — | 1 | - |
| CHEMBL2071195 | — | — | 1 | - |
| CHEMBL2071271 | — | — | 1 | - |
| CHEMBL2071196 | — | — | 1 | - |
| CHEMBL2071197 | — | — | 1 | - |
| CHEMBL2071198 | — | — | 1 | - |
| CHEMBL2071215 | — | — | 1 | - |
| CHEMBL2071214 | — | — | 1 | - |
| CHEMBL2071213 | — | — | 1 | - |
| CHEMBL2071212 | — | — | 1 | - |
| CHEMBL2071211 | — | — | 1 | - |
| CHEMBL2071209 | — | — | 1 | - |
| CHEMBL2071208 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1980297 | ILORASERTIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2071216 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2071201 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1614709 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2071202 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2071200 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2071217 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2071276 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2071270 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2071277 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2071275 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2071203 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2071274 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2071210 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2071273 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2071272 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL2071204 | — | IC50 | - | — | - | |
| CHEMBL2071205 | — | IC50 | - | — | - | |
| CHEMBL2071206 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2071207 | — | IC50 | - | — | - | |
| CHEMBL2071208 | — | IC50 | - | — | - | |
| CHEMBL2071209 | — | IC50 | - | — | - | |
| CHEMBL2071211 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2071212 | — | IC50 | - | — | - | |
| CHEMBL2071213 | — | IC50 | - | — | - | |
| CHEMBL2071214 | — | IC50 | - | — | - | |
| CHEMBL2071215 | — | IC50 | - | — | - | |
| CHEMBL2071198 | — | IC50 | - | — | - | |
| CHEMBL2071197 | — | IC50 | - | — | - | |
| CHEMBL2071196 | — | IC50 | - | — | - | |
| CHEMBL2071271 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2071195 | — | IC50 | - | — | - | |
| CHEMBL2071199 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2071194 | — | IC50 | - | — | - |