Assay Detail
Binding
CHEMBL3705409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Inhibition Assay: The FGFR2-inhibiting activity was measured based on the activity to inhibit phosphorylation of the biotinylated peptide EGPWLEEEEEAYGWMDF by the human FGFR2 enzyme prepared using a baculovirus expression system. Phosphorylated biotinylated peptides were detected by the time-resolved fluorescent measurement using a europium cryptate-linked anti-phophotyrosine antibody and a streptavidin to which XL665, a derivative of allophycocyanine, is linked. The 50% inhibitory concentration (IC50) was calculated based on the inhibitory rate against the control group without test substances.
111
Total Activities
111
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
Aminopyrazole derivative
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 111 | 7.63 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3676315 | — | — | 1 | 8.49 |
| CHEMBL3681278 | — | — | 1 | 8.47 |
| CHEMBL3681294 | — | — | 1 | 8.44 |
| CHEMBL3681284 | — | — | 1 | 8.40 |
| CHEMBL3681303 | — | — | 1 | 8.40 |
| CHEMBL3676316 | — | — | 1 | 8.37 |
| CHEMBL3676328 | — | — | 1 | 8.37 |
| CHEMBL3681292 | — | — | 1 | 8.34 |
| CHEMBL3681291 | — | — | 1 | 8.32 |
| CHEMBL3676320 | — | — | 1 | 8.27 |
| CHEMBL3676313 | — | — | 1 | 8.26 |
| CHEMBL3681250 | — | — | 1 | 8.26 |
| CHEMBL3681307 | — | — | 1 | 8.26 |
| CHEMBL3676314 | — | — | 1 | 8.25 |
| CHEMBL3681282 | — | — | 1 | 8.22 |
| CHEMBL3681264 | — | — | 1 | 8.21 |
| CHEMBL3681290 | — | — | 1 | 8.20 |
| CHEMBL3681306 | — | — | 1 | 8.12 |
| CHEMBL3681248 | — | — | 1 | 8.08 |
| CHEMBL3681270 | — | — | 1 | 8.08 |
| CHEMBL3676317 | — | — | 1 | 8.07 |
| CHEMBL3676331 | — | — | 1 | 8.07 |
| CHEMBL3681272 | — | — | 1 | 8.07 |
| CHEMBL3676329 | — | — | 1 | 8.05 |
| CHEMBL3681285 | — | — | 1 | 8.04 |
| CHEMBL3681314 | — | — | 1 | 8.03 |
| CHEMBL3681246 | — | — | 1 | 8.00 |
| CHEMBL3681295 | — | — | 1 | 8.00 |
| CHEMBL3681258 | — | — | 1 | 8.00 |
| CHEMBL3681289 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3676315 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3681278 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3681294 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3681303 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3681284 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3676316 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3676328 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3681292 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3681291 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3676320 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3676313 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3681307 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3681250 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3676314 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3681282 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3681264 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3681290 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3681306 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3681270 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3681248 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3676317 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3676331 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3681272 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3676329 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3681285 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3681314 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3681258 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3681246 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3681295 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3681289 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3676325 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681280 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681274 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681236 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681271 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681247 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3681249 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3681251 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3681298 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3681296 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3676324 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3681304 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3676337 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3681240 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3681267 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3681256 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3676327 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3681316 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3681263 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3681281 | — | IC50 | = | 19.0 | nM | 7.72 |