Assay Detail
Binding
CHEMBL1252157
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Inhibition of VEGFR2 expressed in human A431 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.29 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1095464 | — | — | 1 | 6.60 |
| CHEMBL1095465 | — | — | 1 | 6.21 |
| CHEMBL276711 | SEMAXANIB | 3.0 | 1 | 4.89 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 4.72 |
| CHEMBL1254199 | — | — | 1 | 4.05 |
| CHEMBL499344 | — | — | 1 | - |
| CHEMBL1254285 | — | — | 1 | - |
| CHEMBL1254286 | — | — | 1 | - |
| CHEMBL1254363 | — | — | 1 | - |
| CHEMBL1254364 | — | — | 1 | - |
| CHEMBL1254443 | — | — | 1 | - |
| CHEMBL1254444 | — | — | 1 | - |
| CHEMBL1254522 | — | — | 1 | - |
| CHEMBL1254523 | — | — | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1095464 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1095465 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL276711 | SEMAXANIB | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL535 | SUNITINIB | IC50 | = | 18900.0 | nM | 4.72 |
| CHEMBL1254199 | — | IC50 | = | 89200.0 | nM | 4.05 |
| CHEMBL499344 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1254285 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254286 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254363 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254364 | — | IC50 | = | 116300.0 | nM | - |
| CHEMBL1254443 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254444 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254522 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL1254523 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | = | 124700.0 | nM | - |