Assay Detail
Binding
CHEMBL4262862
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Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay
9
Total Activities
9
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 |
Publication
Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.72 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4284069 | — | — | 1 | 8.82 |
| CHEMBL4279514 | — | — | 1 | 8.66 |
| CHEMBL4068896 | — | — | 1 | 7.85 |
| CHEMBL2403844 | — | — | 1 | 7.54 |
| CHEMBL4294665 | — | — | 1 | 7.28 |
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 7.25 |
| CHEMBL4277111 | — | — | 1 | 7.24 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 7.15 |
| CHEMBL509032 | TAE-684 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4284069 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4279514 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4068896 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2403844 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4294665 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4277111 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL509032 | TAE-684 | IC50 | - | — | - |