Assay Detail
Binding
CHEMBL4417512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human FGFR1 cytoplasmic domain (398-822 AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay
4
Total Activities
4
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 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.80 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 9.23 |
| CHEMBL4548481 | — | — | 1 | 6.09 |
| CHEMBL4439933 | — | — | 1 | 5.96 |
| CHEMBL4537004 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4548481 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL4439933 | — | IC50 | = | 1103.0 | nM | 5.96 |
| CHEMBL4537004 | — | IC50 | = | 1217.0 | nM | 5.92 |