Assay Detail
Binding
CHEMBL864248
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Inhibition of KDR
20
Total Activities
20
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
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.71 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196363 | — | — | 1 | 8.52 |
| CHEMBL213504 | — | — | 1 | 8.40 |
| CHEMBL445570 | — | — | 1 | 8.30 |
| CHEMBL262433 | — | — | 1 | 8.10 |
| CHEMBL376951 | — | — | 1 | 7.89 |
| CHEMBL214258 | — | — | 1 | 7.80 |
| CHEMBL379372 | — | — | 1 | 7.72 |
| CHEMBL210003 | — | — | 1 | 7.62 |
| CHEMBL213505 | — | — | 1 | 7.16 |
| CHEMBL211378 | — | — | 1 | 7.01 |
| CHEMBL378687 | — | — | 1 | 6.65 |
| CHEMBL378941 | — | — | 1 | 5.68 |
| CHEMBL213510 | — | — | 1 | 5.07 |
| CHEMBL540203 | — | — | 1 | 4.80 |
| CHEMBL387300 | — | — | 1 | 4.66 |
| CHEMBL211327 | — | — | 1 | 4.37 |
| CHEMBL374206 | — | — | 1 | 4.34 |
| CHEMBL211379 | — | — | 1 | - |
| CHEMBL213862 | — | — | 1 | - |
| CHEMBL374631 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196363 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL213504 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL445570 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL262433 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL376951 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL214258 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL379372 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL210003 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL213505 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL211378 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL378687 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL378941 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL213510 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL540203 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL387300 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL211327 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL374206 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL211379 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL213862 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL374631 | — | IC50 | > | 50000.0 | nM | - |