Assay Detail
Binding
CHEMBL5100328
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type partial length human FLT3 (V592 to Y969 residues) expressed in bacterial expression system using Ulight-p70S6K peptide substrate incubated for 90 mins in presence of ATP by HTRF assay
8
Total Activities
8
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
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.16 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5202408 | — | — | 1 | 8.10 |
| CHEMBL5201556 | — | — | 1 | 7.92 |
| CHEMBL5200643 | — | — | 1 | 7.60 |
| CHEMBL5206837 | — | — | 1 | 7.01 |
| CHEMBL5184953 | — | — | 1 | 7.01 |
| CHEMBL5187371 | — | — | 1 | 6.94 |
| CHEMBL5174279 | — | — | 1 | 6.81 |
| CHEMBL5208443 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5202408 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5201556 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5200643 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5206837 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5184953 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5187371 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5174279 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5208443 | — | IC50 | = | 1343.0 | nM | 5.87 |