Assay Detail
Binding
CHEMBL3778240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KIF5B/RET (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 | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET (CHEMBL3430888) ↗| Type | CHIMERIC 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 | 6.15 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440727 | — | — | 1 | 7.39 |
| CHEMBL3775169 | — | — | 1 | 7.28 |
| CHEMBL3774904 | — | — | 1 | 7.28 |
| CHEMBL3774489 | — | — | 1 | 7.07 |
| CHEMBL3775557 | — | — | 1 | 6.92 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.72 |
| CHEMBL3775934 | — | — | 1 | 6.70 |
| CHEMBL3774953 | — | — | 1 | 6.58 |
| CHEMBL3775511 | — | — | 1 | 6.57 |
| CHEMBL127907 | — | — | 1 | 6.42 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.40 |
| CHEMBL3774951 | — | — | 1 | 6.34 |
| CHEMBL3775560 | — | — | 1 | 6.34 |
| CHEMBL3775879 | — | — | 1 | 6.31 |
| CHEMBL478442 | — | — | 1 | 6.30 |
| CHEMBL3775903 | — | — | 1 | 6.24 |
| CHEMBL3775672 | — | — | 1 | 6.21 |
| CHEMBL235851 | — | — | 1 | 6.03 |
| CHEMBL3774580 | — | — | 1 | 5.96 |
| CHEMBL3775190 | — | — | 1 | 5.85 |
| CHEMBL3775086 | — | — | 1 | 5.82 |
| CHEMBL1277620 | — | — | 1 | 5.77 |
| CHEMBL3775840 | — | — | 1 | 5.72 |
| CHEMBL3774563 | — | — | 1 | 5.72 |
| CHEMBL3775376 | — | — | 1 | 5.70 |
| CHEMBL3775336 | — | — | 1 | 5.70 |
| CHEMBL3774913 | — | — | 1 | 5.68 |
| CHEMBL3775940 | — | — | 1 | 5.68 |
| CHEMBL3775585 | — | — | 1 | 5.66 |
| CHEMBL3775164 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440727 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3775169 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3774904 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3774489 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3775557 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3775934 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3774953 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3775511 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL127907 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3774951 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3775560 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3775879 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL478442 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3775903 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3775672 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL235851 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3774580 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3775190 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3775086 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1277620 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3775840 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3774563 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3775376 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3775336 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3774913 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3775940 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3775585 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3775164 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3774697 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3774430 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL3775569 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3774935 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3774623 | — | IC50 | - | — | - |