Assay Detail
Binding
CHEMBL1010124
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Inhibition of human recombinant VEGFR2
40
Total Activities
40
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, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.92 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495749 | — | — | 1 | 8.30 |
| CHEMBL495763 | — | — | 1 | 7.92 |
| CHEMBL498013 | — | — | 1 | 7.85 |
| CHEMBL495762 | — | — | 1 | 7.85 |
| CHEMBL498551 | — | — | 1 | 7.77 |
| CHEMBL496764 | — | — | 1 | 7.72 |
| CHEMBL495735 | — | — | 1 | 7.68 |
| CHEMBL498214 | — | — | 1 | 7.58 |
| CHEMBL495961 | — | — | 1 | 7.57 |
| CHEMBL495962 | — | — | 1 | 7.54 |
| CHEMBL204427 | — | — | 1 | 7.38 |
| CHEMBL523745 | — | — | 1 | 7.37 |
| CHEMBL526507 | — | — | 1 | 7.30 |
| CHEMBL496762 | — | — | 1 | 7.28 |
| CHEMBL383417 | — | — | 1 | 7.24 |
| CHEMBL204426 | — | — | 1 | 7.24 |
| CHEMBL496150 | — | — | 1 | 7.22 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.19 |
| CHEMBL523071 | — | — | 1 | 7.18 |
| CHEMBL526658 | — | — | 1 | 7.18 |
| CHEMBL496763 | — | — | 1 | 7.11 |
| CHEMBL498347 | — | — | 1 | 6.89 |
| CHEMBL495529 | — | — | 1 | 6.80 |
| CHEMBL495984 | — | — | 1 | 6.77 |
| CHEMBL522732 | — | — | 1 | 6.72 |
| CHEMBL498206 | — | — | 1 | 6.68 |
| CHEMBL521552 | — | — | 1 | 6.66 |
| CHEMBL498205 | — | — | 1 | 6.66 |
| CHEMBL377345 | — | — | 1 | 6.62 |
| CHEMBL526836 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495749 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL495763 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL495762 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL498013 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL498551 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL496764 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL495735 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL498214 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL495961 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL495962 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL204427 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL523745 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL526507 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL496762 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL204426 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL383417 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL496150 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL523071 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL526658 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL496763 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL498347 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL495529 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL495984 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL522732 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL498206 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL521552 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL498205 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL377345 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL526836 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL495983 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL526285 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL495530 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL449593 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL118440 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL498348 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL523571 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL457985 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL496173 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL496172 | — | IC50 | > | 25000.0 | nM | - |