Assay Detail
Binding
CHEMBL3778238
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 | 44 | 6.59 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440727 | — | — | 1 | 8.64 |
| CHEMBL3775169 | — | — | 1 | 8.02 |
| CHEMBL3775190 | — | — | 1 | 7.82 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.80 |
| CHEMBL3775415 | — | — | 1 | 7.77 |
| CHEMBL478442 | — | — | 1 | 7.75 |
| CHEMBL3774904 | — | — | 1 | 7.70 |
| CHEMBL235851 | — | — | 1 | 7.24 |
| CHEMBL3775934 | — | — | 1 | 7.18 |
| CHEMBL127907 | — | — | 1 | 7.18 |
| CHEMBL3775557 | — | — | 1 | 7.16 |
| CHEMBL3774489 | — | — | 1 | 7.15 |
| CHEMBL3774563 | — | — | 1 | 7.14 |
| CHEMBL3775879 | — | — | 1 | 7.14 |
| CHEMBL3775672 | — | — | 1 | 6.82 |
| CHEMBL3774951 | — | — | 1 | 6.80 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.76 |
| CHEMBL3775376 | — | — | 1 | 6.68 |
| CHEMBL3775336 | — | — | 1 | 6.64 |
| CHEMBL3775511 | — | — | 1 | 6.64 |
| CHEMBL3775903 | — | — | 1 | 6.55 |
| CHEMBL3775086 | — | — | 1 | 6.46 |
| CHEMBL3775560 | — | — | 1 | 6.44 |
| CHEMBL1277620 | — | — | 1 | 6.34 |
| CHEMBL3774953 | — | — | 1 | 5.96 |
| CHEMBL3775585 | — | — | 1 | 5.85 |
| CHEMBL3774580 | — | — | 1 | 5.64 |
| CHEMBL3775840 | — | — | 1 | 5.60 |
| CHEMBL405130 | WHI-P131 | 1.0 | 1 | 5.55 |
| CHEMBL3775164 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440727 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3775169 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3775190 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3775415 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL478442 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3774904 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL235851 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3775934 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL127907 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3775557 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3774489 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3774563 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3775879 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3775672 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3774951 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL3775376 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3775336 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3775511 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3775903 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3775086 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3775560 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1277620 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3774953 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3775585 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3774580 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3775840 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL405130 | WHI-P131 | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3775164 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3774935 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL169473 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3775940 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3774913 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3220401 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3774430 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL3775240 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774623 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774697 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774643 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774720 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3774450 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775569 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3775660 | — | IC50 | > | 10000.0 | nM | - |