Assay Detail
Binding
CHEMBL2032454
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Inhibition of VEGFR2 by HTRF assay
50
Total Activities
48
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 6.39 | 8.11 |
| IC50 | 2 | 7.00 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2031893 | — | — | 2 | 8.11 |
| CHEMBL2031900 | — | — | 1 | 7.74 |
| CHEMBL460465 | — | — | 1 | 7.62 |
| CHEMBL2031898 | — | — | 1 | 7.45 |
| CHEMBL2031896 | — | — | 1 | 7.42 |
| CHEMBL2031901 | — | — | 1 | 7.38 |
| CHEMBL2032023 | — | — | 1 | 7.13 |
| CHEMBL2031894 | — | — | 1 | 7.10 |
| CHEMBL2031912 | — | — | 1 | 6.88 |
| CHEMBL460466 | — | — | 1 | 6.79 |
| CHEMBL2032025 | — | — | 1 | 6.72 |
| CHEMBL2032020 | — | — | 1 | 6.68 |
| CHEMBL2032026 | — | — | 1 | 6.63 |
| CHEMBL2029375 | — | — | 1 | 6.61 |
| CHEMBL2032028 | — | — | 1 | 6.59 |
| CHEMBL2032022 | — | — | 1 | 6.51 |
| CHEMBL2032027 | — | — | 1 | 6.49 |
| CHEMBL2032021 | — | — | 1 | 6.46 |
| CHEMBL2032031 | — | — | 1 | 6.42 |
| CHEMBL460468 | — | — | 1 | 6.41 |
| CHEMBL2032030 | — | — | 1 | 6.41 |
| CHEMBL518174 | — | — | 1 | 6.40 |
| CHEMBL2032024 | — | — | 1 | 6.34 |
| CHEMBL2032018 | — | — | 1 | 6.30 |
| CHEMBL2032032 | — | — | 1 | 6.29 |
| CHEMBL2031903 | — | — | 1 | 6.27 |
| CHEMBL2032019 | — | — | 1 | 6.23 |
| CHEMBL2031899 | — | — | 1 | 6.15 |
| CHEMBL2031911 | — | — | 1 | 6.15 |
| CHEMBL2031905 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2031893 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL2031893 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2031900 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL460465 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL2031898 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL2031896 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL2031901 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2032023 | — | Ki | = | 74.1 | nM | 7.13 |
| CHEMBL2031894 | — | Ki | = | 78.9 | nM | 7.10 |
| CHEMBL2031912 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL460466 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL2032025 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL2032020 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL2032026 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL2029375 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL2032028 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL2032022 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL2032027 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL2032021 | — | Ki | = | 343.0 | nM | 6.46 |
| CHEMBL2032031 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL460468 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL2032030 | — | Ki | = | 389.0 | nM | 6.41 |
| CHEMBL518174 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL2032024 | — | Ki | = | 452.0 | nM | 6.34 |
| CHEMBL2032018 | — | Ki | = | 501.0 | nM | 6.30 |
| CHEMBL2032032 | — | Ki | = | 519.0 | nM | 6.29 |
| CHEMBL2031903 | — | Ki | = | 541.0 | nM | 6.27 |
| CHEMBL2032019 | — | Ki | = | 588.0 | nM | 6.23 |
| CHEMBL2031899 | — | Ki | = | 702.0 | nM | 6.15 |
| CHEMBL2031911 | — | Ki | = | 708.0 | nM | 6.15 |
| CHEMBL2031905 | — | Ki | = | 903.0 | nM | 6.04 |
| CHEMBL2032029 | — | Ki | = | 932.0 | nM | 6.03 |
| CHEMBL2031913 | — | Ki | = | 945.0 | nM | 6.03 |
| CHEMBL459647 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL460472 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL445799 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL2031904 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL2031906 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL2032015 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL2031902 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL2031907 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL2031897 | — | Ki | = | 1980.0 | nM | 5.70 |
| CHEMBL2031909 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL460472 | — | Ki | = | 2430.0 | nM | 5.61 |
| CHEMBL2032013 | — | Ki | = | 2720.0 | nM | 5.57 |
| CHEMBL2032016 | — | Ki | = | 2830.0 | nM | 5.55 |
| CHEMBL2031908 | — | Ki | = | 3350.0 | nM | 5.47 |
| CHEMBL2032017 | — | Ki | = | 4730.0 | nM | 5.33 |
| CHEMBL2031910 | — | Ki | > | 6600.0 | nM | - |
| CHEMBL2032014 | — | Ki | > | 6600.0 | nM | - |