Assay Detail
Binding
CHEMBL853495
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Inhibition of KDR by HTRF kinase assay
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 aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.43 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215943 | — | — | 1 | 9.00 |
| CHEMBL212964 | — | — | 1 | 9.00 |
| CHEMBL385937 | — | — | 1 | 8.70 |
| CHEMBL215019 | — | — | 1 | 8.52 |
| CHEMBL215863 | — | — | 1 | 8.40 |
| CHEMBL212128 | — | — | 1 | 8.30 |
| CHEMBL212181 | — | — | 1 | 8.22 |
| CHEMBL214530 | — | — | 1 | 8.15 |
| CHEMBL215969 | — | — | 1 | 8.10 |
| CHEMBL427226 | — | — | 1 | 8.10 |
| CHEMBL213290 | — | — | 1 | 7.82 |
| CHEMBL215813 | — | — | 1 | 7.82 |
| CHEMBL386661 | — | — | 1 | 7.77 |
| CHEMBL212183 | — | — | 1 | 7.68 |
| CHEMBL213831 | — | — | 1 | 7.33 |
| CHEMBL427233 | — | — | 1 | 7.32 |
| CHEMBL424719 | — | — | 1 | 7.28 |
| CHEMBL215691 | — | — | 1 | 6.99 |
| CHEMBL384942 | — | — | 1 | 6.76 |
| CHEMBL214556 | — | — | 1 | 6.61 |
| CHEMBL212195 | — | — | 1 | 6.54 |
| CHEMBL212953 | — | — | 1 | 6.51 |
| CHEMBL385055 | — | — | 1 | 6.44 |
| CHEMBL385598 | — | — | 1 | 6.34 |
| CHEMBL214495 | — | — | 1 | 5.85 |
| CHEMBL213478 | — | — | 1 | 5.84 |
| CHEMBL215952 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215943 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL212964 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL385937 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL215019 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL215863 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL212128 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL212181 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL214530 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL215969 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL427226 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL213290 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL215813 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL386661 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL212183 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL213831 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL427233 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL424719 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL215691 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL384942 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL214556 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL212195 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL212953 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL385055 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL385598 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL214495 | — | IC50 | = | 1415.0 | nM | 5.85 |
| CHEMBL213478 | — | IC50 | = | 1438.0 | nM | 5.84 |
| CHEMBL215952 | — | IC50 | = | 4966.0 | nM | 5.30 |