Assay Detail
Binding
CHEMBL4834259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay
12
Total Activities
12
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
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.94 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL169390 | — | — | 1 | 8.15 |
| CHEMBL4858720 | — | — | 1 | 7.96 |
| CHEMBL4874648 | — | — | 1 | 7.82 |
| CHEMBL4857808 | — | — | 1 | 7.70 |
| CHEMBL4859681 | — | — | 1 | 7.66 |
| CHEMBL4877264 | — | — | 1 | 7.36 |
| CHEMBL4853155 | — | — | 1 | 7.05 |
| CHEMBL4854822 | — | — | 1 | 6.62 |
| CHEMBL4848347 | — | — | 1 | 6.11 |
| CHEMBL4855562 | — | — | 1 | 5.72 |
| CHEMBL4864386 | — | — | 1 | 5.55 |
| CHEMBL4860822 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL169390 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4858720 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4874648 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4857808 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4859681 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4877264 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4853155 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4854822 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4848347 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4855562 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4864386 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4860822 | — | IC50 | = | 3000.0 | nM | 5.52 |