Assay Detail
Binding
CHEMBL4188978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type human partial length VEGFR2 (R787 to P1253 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP
14
Total Activities
14
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
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.03 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | 2.0 | 1 | 8.10 |
| CHEMBL4218175 | — | — | 1 | 7.18 |
| CHEMBL4208852 | — | — | 1 | 6.40 |
| CHEMBL4213003 | — | — | 1 | 6.16 |
| CHEMBL4213775 | — | — | 1 | 5.72 |
| CHEMBL4214476 | — | — | 1 | 5.35 |
| CHEMBL4218369 | — | — | 1 | 5.12 |
| CHEMBL4209569 | — | — | 1 | 5.12 |
| CHEMBL4217649 | — | — | 1 | 5.11 |
| CHEMBL4204515 | — | — | 1 | - |
| CHEMBL4207004 | — | — | 1 | - |
| CHEMBL4211308 | — | — | 1 | - |
| CHEMBL4205191 | — | — | 1 | - |
| CHEMBL4210084 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4218175 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4208852 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4213003 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4213775 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4214476 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4218369 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4209569 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4217649 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4204515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4207004 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4211308 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4205191 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4210084 | — | IC50 | > | 10000.0 | nM | - |