Assay Detail
Binding
CHEMBL1250641
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Inhibition of human VEGFR2
27
Total Activities
27
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
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.89 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1254923 | — | — | 1 | 8.57 |
| CHEMBL1254190 | — | — | 1 | 8.43 |
| CHEMBL1254670 | — | — | 1 | 8.39 |
| CHEMBL1254835 | — | — | 1 | 8.36 |
| CHEMBL1254753 | — | — | 1 | 8.28 |
| CHEMBL1254007 | — | — | 1 | 8.21 |
| CHEMBL1254096 | — | — | 1 | 8.15 |
| CHEMBL1254276 | — | — | 1 | 7.85 |
| CHEMBL1254836 | — | — | 1 | 7.72 |
| CHEMBL1254191 | — | — | 1 | 7.52 |
| CHEMBL1254752 | — | — | 1 | 7.50 |
| CHEMBL1254511 | — | — | 1 | 7.48 |
| CHEMBL1254002 | — | — | 1 | 6.96 |
| CHEMBL1254669 | — | — | 1 | 6.47 |
| CHEMBL1255011 | — | — | 1 | 6.06 |
| CHEMBL1255010 | — | — | 1 | 6.03 |
| CHEMBL1254003 | — | — | 1 | 5.85 |
| CHEMBL1254924 | — | — | 1 | 5.75 |
| CHEMBL1253834 | — | — | 1 | 5.48 |
| CHEMBL1254591 | — | — | 1 | 5.41 |
| CHEMBL1253915 | — | — | 1 | 5.38 |
| CHEMBL1254590 | — | — | 1 | 5.20 |
| CHEMBL1253914 | — | — | 1 | 5.17 |
| CHEMBL1255093 | — | — | 1 | 5.03 |
| CHEMBL1253833 | — | — | 1 | - |
| CHEMBL1255094 | — | — | 1 | - |
| CHEMBL1254095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1254923 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1254190 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1254670 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1254835 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1254753 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1254007 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1254096 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL1254276 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1254836 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1254191 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1254752 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1254511 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1254002 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1254669 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1255011 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1255010 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1254003 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1254924 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1253834 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1254591 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1253915 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1254590 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1253914 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1255093 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL1253833 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1255094 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1254095 | — | IC50 | > | 10000.0 | nM | - |