Assay Detail
Binding
CHEMBL4262868
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 12 | 7.45 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4279514 | — | — | 1 | 8.12 |
| CHEMBL4068896 | — | — | 1 | 8.03 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.70 |
| CHEMBL4294665 | — | — | 1 | 7.68 |
| CHEMBL4277111 | — | — | 1 | 7.37 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 7.19 |
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 7.17 |
| CHEMBL4284069 | — | — | 1 | 6.35 |
| CHEMBL4285284 | — | — | 1 | - |
| CHEMBL4289718 | — | — | 1 | - |
| CHEMBL4281847 | — | — | 1 | - |
| CHEMBL59799 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4279514 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4068896 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL509032 | TAE-684 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4294665 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4277111 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4284069 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL4285284 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4289718 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4281847 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL59799 | — | IC50 | > | 10000.0 | nM | - |