Assay Detail
Binding
CHEMBL929873
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Inhibition of human recombinant VEGFR2 by HTRF assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.15 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404322 | — | — | 1 | 9.00 |
| CHEMBL258014 | — | — | 1 | 9.00 |
| CHEMBL257789 | — | — | 1 | 9.00 |
| CHEMBL404718 | — | — | 1 | 8.70 |
| CHEMBL401860 | — | — | 1 | 8.52 |
| CHEMBL258000 | — | — | 1 | 8.52 |
| CHEMBL257788 | — | — | 1 | 8.40 |
| CHEMBL257793 | — | — | 1 | 8.40 |
| CHEMBL255283 | — | — | 1 | 8.40 |
| CHEMBL401876 | — | — | 1 | 8.40 |
| CHEMBL428433 | — | — | 1 | 8.40 |
| CHEMBL401896 | — | — | 1 | 8.40 |
| CHEMBL255282 | — | — | 1 | 8.30 |
| CHEMBL258015 | — | — | 1 | 8.15 |
| CHEMBL258433 | — | — | 1 | 8.00 |
| CHEMBL429138 | — | — | 1 | 7.96 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 7.96 |
| CHEMBL403606 | — | — | 1 | 7.92 |
| CHEMBL257787 | — | — | 1 | 7.75 |
| CHEMBL257794 | — | — | 1 | 7.64 |
| CHEMBL401897 | — | — | 1 | 7.62 |
| CHEMBL403823 | — | — | 1 | 7.51 |
| CHEMBL255281 | — | — | 1 | 7.51 |
| CHEMBL258436 | — | — | 1 | 7.29 |
| CHEMBL258222 | — | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404322 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL258014 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL257789 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL404718 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL401860 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL258000 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL257788 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL257793 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL255283 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL401876 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL428433 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL401896 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL255282 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL258015 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL258433 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL429138 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL253969 | OSI-632 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL403606 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL257787 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL257794 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL401897 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL403823 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL255281 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL258436 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL258222 | — | IC50 | = | 94.0 | nM | 7.03 |