Assay Detail
Binding
CHEMBL5100323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 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
30
Total Activities
30
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 | 30 | 8.17 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175256 | — | — | 1 | 9.70 |
| CHEMBL5203027 | — | — | 1 | 9.40 |
| CHEMBL5180631 | — | — | 1 | 9.30 |
| CHEMBL5189383 | — | — | 1 | 9.22 |
| CHEMBL5174279 | — | — | 1 | 9.22 |
| CHEMBL5206837 | — | — | 1 | 9.15 |
| CHEMBL5184953 | — | — | 1 | 9.05 |
| CHEMBL5200643 | — | — | 1 | 9.05 |
| CHEMBL5199231 | — | — | 1 | 9.00 |
| CHEMBL5202943 | — | — | 1 | 8.96 |
| CHEMBL5187371 | — | — | 1 | 8.89 |
| CHEMBL4297522 | PEMIGATINIB | 4.0 | 1 | 8.77 |
| CHEMBL5208443 | — | — | 1 | 8.66 |
| CHEMBL5196280 | — | — | 1 | 8.62 |
| CHEMBL5172121 | — | — | 1 | 8.59 |
| CHEMBL5202408 | — | — | 1 | 8.59 |
| CHEMBL1852688 | INFIGRATINIB | 4.0 | 1 | 8.57 |
| CHEMBL5201556 | — | — | 1 | 8.34 |
| CHEMBL5176738 | — | — | 1 | 7.89 |
| CHEMBL5169540 | — | — | 1 | 7.75 |
| CHEMBL5170079 | — | — | 1 | 7.47 |
| CHEMBL5179197 | — | — | 1 | 7.39 |
| CHEMBL5170742 | — | — | 1 | 7.27 |
| CHEMBL5180065 | — | — | 1 | 7.25 |
| CHEMBL5189074 | — | — | 1 | 7.17 |
| CHEMBL5184462 | — | — | 1 | 6.78 |
| CHEMBL5190948 | — | — | 1 | 6.61 |
| CHEMBL5181232 | — | — | 1 | 6.36 |
| CHEMBL5204157 | — | — | 1 | 6.29 |
| CHEMBL5170159 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175256 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5203027 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5180631 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5189383 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5174279 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5206837 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5184953 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5200643 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5199231 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5202943 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5187371 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4297522 | PEMIGATINIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5208443 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5196280 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5172121 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5202408 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1852688 | INFIGRATINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5201556 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5176738 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5169540 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5170079 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5179197 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5170742 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5180065 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5189074 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5184462 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL5190948 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL5181232 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL5204157 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL5170159 | — | IC50 | = | 1177.0 | nM | 5.93 |