Assay Detail
Binding
CHEMBL3705582
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: 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 .mu.M), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 .mu.M), 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.degree. C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer.
52
Total Activities
50
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
3,5-disubstituted alkynylbenzene compound and salt thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 8.32 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3701256 | — | — | 1 | 9.40 |
| CHEMBL3701258 | — | — | 2 | 9.40 |
| CHEMBL3701268 | — | — | 1 | 9.22 |
| CHEMBL3701275 | — | — | 1 | 9.00 |
| CHEMBL3701267 | — | — | 2 | 9.00 |
| CHEMBL3701238 | FUTIBATINIB | 4.0 | 1 | 8.96 |
| CHEMBL3701239 | — | — | 1 | 8.96 |
| CHEMBL3701241 | — | — | 1 | 8.96 |
| CHEMBL3701279 | — | — | 1 | 8.92 |
| CHEMBL3701242 | — | — | 1 | 8.92 |
| CHEMBL3701271 | — | — | 1 | 8.92 |
| CHEMBL3701272 | — | — | 1 | 8.82 |
| CHEMBL3701270 | — | — | 1 | 8.82 |
| CHEMBL3701262 | — | — | 1 | 8.70 |
| CHEMBL3701243 | — | — | 1 | 8.66 |
| CHEMBL3701273 | — | — | 1 | 8.64 |
| CHEMBL3701237 | — | — | 1 | 8.62 |
| CHEMBL3701269 | — | — | 1 | 8.60 |
| CHEMBL3701249 | — | — | 1 | 8.57 |
| CHEMBL3701245 | — | — | 1 | 8.52 |
| CHEMBL3701259 | — | — | 1 | 8.49 |
| CHEMBL3701250 | — | — | 1 | 8.48 |
| CHEMBL3701254 | — | — | 1 | 8.43 |
| CHEMBL3701244 | — | — | 1 | 8.42 |
| CHEMBL3701246 | — | — | 1 | 8.42 |
| CHEMBL3701247 | — | — | 1 | 8.39 |
| CHEMBL3701261 | — | — | 1 | 8.37 |
| CHEMBL3701248 | — | — | 1 | 8.37 |
| CHEMBL3701257 | — | — | 1 | 8.33 |
| CHEMBL3701251 | — | — | 1 | 8.25 |
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 |
| CHEMBL3701242 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3701271 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3701279 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3701272 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3701267 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3701270 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3701262 | — | 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 |
| CHEMBL3701269 | — | 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 |
| CHEMBL3701250 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3701254 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3701246 | — | 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 |
| CHEMBL3701257 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3701258 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3701251 | — | 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 |
| CHEMBL3701264 | — | 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 |
| CHEMBL3701280 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3701255 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3701285 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3701282 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3701284 | — | 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 |
| CHEMBL3701278 | — | IC50 | < | 0.3 | nM | - |