Assay Detail
Binding
CHEMBL5731622
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FGFR2 Kinase Activity: When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences, Inc.) was used as a substrate. The purified recombinant human FGFR2 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration that was 20 times higher than the final concentration. Next, the purified human FGFR2 protein, FL-Peptide 22 (final concentration: 1.5 μM), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 μM), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer (15 mM Tris-HCl pH 7.5, 0.01% Tween-20, 2 mM DTT), and the mixture was incubated at 25° C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer (Caliper Life Sciences, Inc.) was added thereto to terminate the kinase reaction. Finally, using a LabChip (registered trademark) 3000 system (Caliper Life Sciences, Inc.; excitation wavelength: 488 nm, detection wavelength: 530 nm), phosphorylated peptides and non-phosphorylated peptides were separated, and the amount of each peptide was measured. The level of phosphorylation was determined from the quantitative ratio. The compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM).
156
Total Activities
49
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Therapeutic agent for FGFR inhibitor-resistant cancer
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 8.32 | 9.40 |
| kon | 52 | - | - |
| k_off | 52 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3701256 | — | — | 3 | 9.40 |
| CHEMBL3701258 | — | — | 3 | 9.40 |
| CHEMBL3701268 | — | — | 3 | 9.22 |
| CHEMBL3701275 | — | — | 3 | 9.00 |
| CHEMBL3701267 | — | — | 3 | 9.00 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 6 | 8.96 |
| CHEMBL3701239 | — | — | 3 | 8.96 |
| CHEMBL3701241 | — | — | 3 | 8.96 |
| CHEMBL6046580 | — | — | 3 | 8.92 |
| CHEMBL3701242 | — | — | 3 | 8.92 |
| CHEMBL3701271 | — | — | 3 | 8.92 |
| CHEMBL3701272 | — | — | 3 | 8.82 |
| CHEMBL3701270 | — | — | 3 | 8.82 |
| CHEMBL6009773 | — | — | 3 | 8.82 |
| CHEMBL5882963 | — | — | 3 | 8.70 |
| CHEMBL3701243 | — | — | 3 | 8.66 |
| CHEMBL3701273 | — | — | 3 | 8.64 |
| CHEMBL3701237 | — | — | 3 | 8.62 |
| CHEMBL5833027 | — | — | 3 | 8.60 |
| CHEMBL3701249 | — | — | 3 | 8.57 |
| CHEMBL3701245 | — | — | 3 | 8.52 |
| CHEMBL3701259 | — | — | 3 | 8.49 |
| CHEMBL5785744 | — | — | 3 | 8.48 |
| CHEMBL5877066 | — | — | 3 | 8.43 |
| CHEMBL6011047 | — | — | 3 | 8.42 |
| CHEMBL3701244 | — | — | 3 | 8.42 |
| CHEMBL3701247 | — | — | 3 | 8.39 |
| CHEMBL3701248 | — | — | 3 | 8.37 |
| CHEMBL3701261 | — | — | 3 | 8.37 |
| CHEMBL5850207 | — | — | 3 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3701256 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3701258 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3701268 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3701267 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3701275 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3701239 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3701241 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3701271 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3701242 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6046580 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3701272 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3701270 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL6009773 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5882963 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3701243 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3701273 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3701237 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5833027 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3701249 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3701245 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3701259 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5785744 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5877066 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL6011047 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3701244 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3701247 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3701261 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3701248 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5850207 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5758512 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3701252 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3701265 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3701260 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3701263 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3701252 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3701240 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3701263 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3701277 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3701253 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3701276 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5948711 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3701255 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3701285 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3701284 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3701238 | FUTIBATINIB | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3701281 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3701286 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3701271 | — | k_off | = | - | s-1 | - |