Assay Detail
Binding
CHEMBL5096259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged FGFR3 (436 to 806 residues) expressed in baculovirus expression system using IGF-1Rtide peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hrs in the presence of ATP by ADP-Glo reagent based luminescence assay
27
Total Activities
27
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 and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.54 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5205436 | — | — | 1 | 8.92 |
| CHEMBL5199374 | — | — | 1 | 8.52 |
| CHEMBL5177815 | — | — | 1 | 8.46 |
| CHEMBL5207255 | — | — | 1 | 8.26 |
| CHEMBL5189958 | — | — | 1 | 8.09 |
| CHEMBL5173892 | — | — | 1 | 8.01 |
| CHEMBL5201819 | — | — | 1 | 7.99 |
| CHEMBL5171314 | — | — | 1 | 7.87 |
| CHEMBL5191338 | — | — | 1 | 7.86 |
| CHEMBL5186357 | — | — | 1 | 7.86 |
| CHEMBL5174735 | — | — | 1 | 7.84 |
| CHEMBL5191301 | — | — | 1 | 7.84 |
| CHEMBL5183603 | — | — | 1 | 7.65 |
| CHEMBL5183691 | — | — | 1 | 7.60 |
| CHEMBL5181778 | — | — | 1 | 7.53 |
| CHEMBL5180534 | — | — | 1 | 7.53 |
| CHEMBL5182544 | — | — | 1 | 7.53 |
| CHEMBL5179660 | — | — | 1 | 7.41 |
| CHEMBL5183701 | — | — | 1 | 7.39 |
| CHEMBL5207581 | — | — | 1 | 7.34 |
| CHEMBL5192921 | — | — | 1 | 7.33 |
| CHEMBL5182130 | — | — | 1 | 6.75 |
| CHEMBL5209158 | — | — | 1 | 6.70 |
| CHEMBL5196797 | — | — | 1 | 6.48 |
| CHEMBL5195888 | — | — | 1 | 6.44 |
| CHEMBL5209163 | — | — | 1 | 6.33 |
| CHEMBL5191065 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5205436 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL5199374 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL5177815 | — | IC50 | = | 3.46 | nM | 8.46 |
| CHEMBL5207255 | — | IC50 | = | 5.51 | nM | 8.26 |
| CHEMBL5189958 | — | IC50 | = | 8.07 | nM | 8.09 |
| CHEMBL5173892 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5201819 | — | IC50 | = | 10.18 | nM | 7.99 |
| CHEMBL5171314 | — | IC50 | = | 13.36 | nM | 7.87 |
| CHEMBL5191338 | — | IC50 | = | 13.93 | nM | 7.86 |
| CHEMBL5186357 | — | IC50 | = | 13.69 | nM | 7.86 |
| CHEMBL5174735 | — | IC50 | = | 14.35 | nM | 7.84 |
| CHEMBL5191301 | — | IC50 | = | 14.56 | nM | 7.84 |
| CHEMBL5183603 | — | IC50 | = | 22.25 | nM | 7.65 |
| CHEMBL5183691 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL5181778 | — | IC50 | = | 29.72 | nM | 7.53 |
| CHEMBL5180534 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL5182544 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL5179660 | — | IC50 | = | 38.98 | nM | 7.41 |
| CHEMBL5183701 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL5207581 | — | IC50 | = | 45.8 | nM | 7.34 |
| CHEMBL5192921 | — | IC50 | = | 46.78 | nM | 7.33 |
| CHEMBL5182130 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL5209158 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL5196797 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL5195888 | — | IC50 | = | 363.55 | nM | 6.44 |
| CHEMBL5209163 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL5191065 | — | IC50 | = | 754.5 | nM | 6.12 |