Assay Detail
ADMET
CHEMBL4262863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of phosphorylated FGFR1 (407 to 822 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 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 | ADMET |
| 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 | 7.36 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | 2.0 | 1 | 9.10 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 9.10 |
| CHEMBL4284069 | — | — | 1 | 8.35 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.72 |
| CHEMBL4279514 | — | — | 1 | 6.55 |
| CHEMBL4068896 | — | — | 1 | 5.50 |
| CHEMBL2403844 | — | — | 1 | 5.20 |
| CHEMBL4277111 | — | — | 1 | - |
| CHEMBL4294665 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3348846 | FEXAGRATINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4284069 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL509032 | TAE-684 | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4279514 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4068896 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2403844 | — | IC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL4277111 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4294665 | — | IC50 | > | 10000.0 | nM | - |