Assay Detail
Binding
CHEMBL829518
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of vascular endothelial growth factor receptor 2
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.47 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188386 | — | — | 1 | 7.20 |
| CHEMBL372657 | — | — | 1 | 7.17 |
| CHEMBL188502 | — | — | 1 | 7.12 |
| CHEMBL365631 | — | — | 1 | 7.12 |
| CHEMBL177688 | — | — | 1 | 7.08 |
| CHEMBL371169 | — | — | 1 | 7.03 |
| CHEMBL190984 | — | — | 1 | 6.98 |
| CHEMBL189226 | — | — | 1 | 6.91 |
| CHEMBL364000 | — | — | 1 | 6.87 |
| CHEMBL189825 | — | — | 1 | 6.78 |
| CHEMBL191107 | — | — | 1 | 6.75 |
| CHEMBL189017 | — | — | 1 | 6.72 |
| CHEMBL189998 | — | — | 1 | 6.63 |
| CHEMBL188901 | — | — | 1 | 6.60 |
| CHEMBL187684 | — | — | 1 | 6.58 |
| CHEMBL188284 | — | — | 1 | 6.56 |
| CHEMBL190960 | — | — | 1 | 6.52 |
| CHEMBL370951 | — | — | 1 | 6.46 |
| CHEMBL188387 | — | — | 1 | 6.41 |
| CHEMBL191160 | — | — | 1 | 6.40 |
| CHEMBL364161 | — | — | 1 | 6.25 |
| CHEMBL363764 | — | — | 1 | 6.23 |
| CHEMBL361898 | — | — | 1 | 6.21 |
| CHEMBL360401 | — | — | 1 | 6.13 |
| CHEMBL189947 | — | — | 1 | 6.00 |
| CHEMBL187571 | — | — | 1 | 6.00 |
| CHEMBL188536 | — | — | 1 | 5.98 |
| CHEMBL189125 | — | — | 1 | 5.87 |
| CHEMBL191251 | — | — | 1 | 5.80 |
| CHEMBL190473 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188386 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL372657 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL365631 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL188502 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL177688 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL371169 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL190984 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL189226 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL364000 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL189825 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL191107 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL189017 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL189998 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL188901 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL187684 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL188284 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL190960 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL370951 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL188387 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL191160 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL364161 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL363764 | — | IC50 | = | 593.0 | nM | 6.23 |
| CHEMBL361898 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL360401 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL189947 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL187571 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL188536 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL189125 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL191251 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL190473 | — | IC50 | = | 2277.0 | nM | 5.64 |
| CHEMBL186412 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL365411 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL364052 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL264769 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL187407 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL188903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL190371 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL188904 | — | IC50 | > | 10000.0 | nM | - |