Assay Detail
Binding
CHEMBL4188977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type human partial length FLT3 (V592 to Y969 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
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| 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 | 7.10 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | 2.0 | 1 | 9.05 |
| CHEMBL4218175 | — | — | 1 | 8.85 |
| CHEMBL4208852 | — | — | 1 | 8.10 |
| CHEMBL4213003 | — | — | 1 | 7.70 |
| CHEMBL4213775 | — | — | 1 | 7.00 |
| CHEMBL4214476 | — | — | 1 | 7.00 |
| CHEMBL4209569 | — | — | 1 | 6.60 |
| CHEMBL4204515 | — | — | 1 | 6.52 |
| CHEMBL4210084 | — | — | 1 | 6.28 |
| CHEMBL4218369 | — | — | 1 | 6.16 |
| CHEMBL4205191 | — | — | 1 | 6.07 |
| CHEMBL4207004 | — | — | 1 | 5.92 |
| CHEMBL4217649 | — | — | 1 | - |
| CHEMBL4211308 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3809489 | BEMCENTINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4218175 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4208852 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4213003 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4213775 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4214476 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4209569 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4204515 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4210084 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4218369 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4205191 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4207004 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4217649 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4211308 | — | IC50 | > | 10000.0 | nM | - |