Assay Detail
Binding
CHEMBL3778241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.31 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440727 | — | — | 1 | 8.02 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.85 |
| CHEMBL3775169 | — | — | 1 | 7.18 |
| CHEMBL478442 | — | — | 1 | 7.06 |
| CHEMBL3774904 | — | — | 1 | 7.01 |
| CHEMBL235851 | — | — | 1 | 6.96 |
| CHEMBL3774489 | — | — | 1 | 6.62 |
| CHEMBL3775934 | — | — | 1 | 6.58 |
| CHEMBL3775190 | — | — | 1 | 6.55 |
| CHEMBL3774563 | — | — | 1 | 6.51 |
| CHEMBL3775879 | — | — | 1 | 6.44 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.20 |
| CHEMBL3775557 | — | — | 1 | 6.11 |
| CHEMBL3775672 | — | — | 1 | 6.08 |
| CHEMBL127907 | — | — | 1 | 6.05 |
| CHEMBL3775560 | — | — | 1 | 6.00 |
| CHEMBL3775086 | — | — | 1 | 5.92 |
| CHEMBL3775903 | — | — | 1 | 5.89 |
| CHEMBL3774951 | — | — | 1 | 5.85 |
| CHEMBL3775376 | — | — | 1 | 5.82 |
| CHEMBL3775511 | — | — | 1 | 5.72 |
| CHEMBL1277620 | — | — | 1 | 5.54 |
| CHEMBL3775336 | — | — | 1 | 5.33 |
| CHEMBL3774953 | — | — | 1 | 5.27 |
| CHEMBL3774580 | — | — | 1 | 5.24 |
| CHEMBL3775569 | — | — | 1 | - |
| CHEMBL3775840 | — | — | 1 | - |
| CHEMBL3775164 | — | — | 1 | - |
| CHEMBL3774913 | — | — | 1 | - |
| CHEMBL3775940 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440727 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3775169 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL478442 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3774904 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL235851 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3774489 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3775934 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3775190 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3774563 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3775879 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3775557 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3775672 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL127907 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL3775560 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3775086 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3775903 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3774951 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3775376 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3775511 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1277620 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3775336 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3774953 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3774580 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3774623 | — | IC50 | - | — | - | |
| CHEMBL3774430 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774935 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775585 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774697 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775940 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774913 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775840 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775569 | — | IC50 | > | 10000.0 | nM | - |