Assay Detail
Binding
CHEMBL3998243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method
12
Total Activities
12
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
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.43 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099682 | — | — | 1 | 7.57 |
| CHEMBL4099329 | — | — | 1 | 7.56 |
| CHEMBL4060996 | — | — | 1 | 7.48 |
| CHEMBL4104515 | — | — | 1 | 7.48 |
| CHEMBL4069672 | — | — | 1 | 7.41 |
| CHEMBL4072383 | — | — | 1 | 7.07 |
| CHEMBL4098409 | — | — | 1 | - |
| CHEMBL67 | COMBRETASTATIN A4 | -1.0 | 1 | - |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL53463 | DOXORUBICIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099682 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL4099329 | — | IC50 | = | 27.3 | nM | 7.56 |
| CHEMBL4060996 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4104515 | — | IC50 | = | 32.9 | nM | 7.48 |
| CHEMBL4069672 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL4072383 | — | IC50 | = | 84.3 | nM | 7.07 |
| CHEMBL4098409 | — | IC50 | > | 200.0 | nM | - |
| CHEMBL67 | COMBRETASTATIN A4 | IC50 | - | — | - | |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12.9 | nM | - |
| CHEMBL535 | SUNITINIB | IC50 | = | 18.9 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | - | — | - | |
| CHEMBL53463 | DOXORUBICIN | IC50 | - | — | - |