Assay Detail
Binding
CHEMBL5100345
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.45 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175256 | — | — | 1 | 9.70 |
| CHEMBL5189383 | — | — | 1 | 9.70 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 9.40 |
| CHEMBL5180631 | — | — | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175256 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5189383 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5180631 | — | IC50 | = | 1.0 | nM | 9.00 |