Assay Detail
Binding
CHEMBL3223151
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Inhibition of KDR catalytic domain (unknown origin) assessed as reduction of poly(Glu:Tyr) substrate phosphorylation after 20 mins by ELISA
16
Total Activities
16
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
Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.95 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL153843 | — | — | 1 | 7.85 |
| CHEMBL3219511 | — | — | 1 | 7.44 |
| CHEMBL3219512 | — | — | 1 | 7.43 |
| CHEMBL3219510 | — | — | 1 | 6.75 |
| CHEMBL3217774 | — | — | 1 | 6.72 |
| CHEMBL3219509 | — | — | 1 | 6.41 |
| CHEMBL3219513 | — | — | 1 | 6.07 |
| CHEMBL3219504 | — | — | 1 | - |
| CHEMBL3219505 | — | — | 1 | - |
| CHEMBL3219502 | — | — | 1 | - |
| CHEMBL3219503 | — | — | 1 | - |
| CHEMBL3218424 | — | — | 1 | - |
| CHEMBL3219506 | — | — | 1 | - |
| CHEMBL3219507 | — | — | 1 | - |
| CHEMBL3219508 | — | — | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL153843 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3219511 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3219512 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3219510 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3217774 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3219509 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3219513 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3219504 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219505 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219502 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219503 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3218424 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219506 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219507 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3219508 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | > | 1000.0 | nM | - |