Assay Detail
Binding
CHEMBL4188980
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type human partial length RET (E713 to D1014 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.63 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | 2.0 | 1 | 8.52 |
| CHEMBL4218175 | — | — | 1 | 8.22 |
| CHEMBL4213003 | — | — | 1 | 7.30 |
| CHEMBL4208852 | — | — | 1 | 7.22 |
| CHEMBL4214476 | — | — | 1 | 6.80 |
| CHEMBL4205191 | — | — | 1 | 6.37 |
| CHEMBL4213775 | — | — | 1 | 6.36 |
| CHEMBL4210084 | — | — | 1 | 6.22 |
| CHEMBL4218369 | — | — | 1 | 6.05 |
| CHEMBL4209569 | — | — | 1 | 5.92 |
| CHEMBL4207004 | — | — | 1 | 5.40 |
| CHEMBL4217649 | — | — | 1 | 5.21 |
| CHEMBL4204515 | — | — | 1 | - |
| CHEMBL4211308 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4218175 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4213003 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4208852 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4214476 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4205191 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4213775 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4210084 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4218369 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4209569 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4207004 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4217649 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4204515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4211308 | — | IC50 | > | 10000.0 | nM | - |