Assay Detail
Binding
CHEMBL5256648
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human EGFR del19/T790M using biotinEEPLYWSFPAKKK-NH2 as substrate incubated for 120 mins by TR-FRET assay
10
Total Activities
10
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
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.94 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5291403 | — | — | 1 | 9.40 |
| CHEMBL5265881 | — | — | 1 | 8.92 |
| CHEMBL5291034 | — | — | 1 | 8.27 |
| CHEMBL5289003 | — | — | 1 | 6.96 |
| CHEMBL5272088 | — | — | 1 | 6.13 |
| CHEMBL5275918 | — | — | 1 | - |
| CHEMBL3701282 | — | — | 1 | - |
| CHEMBL5284165 | — | — | 1 | - |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | - |
| CHEMBL5273555 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5291403 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5265881 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5291034 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5289003 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5272088 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL5275918 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3701282 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5284165 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3701238 | FUTIBATINIB | IC50 | > | 5000.0 | nM | - |
| CHEMBL5273555 | — | IC50 | > | 5000.0 | nM | - |