Assay Detail
Binding
CHEMBL4013829
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR1 in HUVEC assessed as reduction in FGF2-induced ERK phosphorylation preincubated for 60 mins followed by FGF2 stimulation for 10 mins by AlphaScreen assay
21
Total Activities
21
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 of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.28 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068509 | PRN-1371 | 1.0 | 1 | 8.96 |
| CHEMBL4099992 | — | — | 1 | 8.92 |
| CHEMBL4089842 | — | — | 1 | 8.89 |
| CHEMBL4066763 | — | — | 1 | 8.80 |
| CHEMBL4061286 | — | — | 1 | 8.80 |
| CHEMBL4088057 | — | — | 1 | 8.66 |
| CHEMBL4092456 | — | — | 1 | 8.62 |
| CHEMBL4099578 | — | — | 1 | 8.47 |
| CHEMBL4095844 | — | — | 1 | 8.39 |
| CHEMBL4061766 | — | — | 1 | 8.25 |
| CHEMBL4095783 | — | — | 1 | 8.22 |
| CHEMBL4081984 | — | — | 1 | 8.11 |
| CHEMBL4064081 | — | — | 1 | 8.07 |
| CHEMBL4102642 | — | — | 1 | 8.03 |
| CHEMBL4083151 | — | — | 1 | 8.02 |
| CHEMBL4084708 | — | — | 1 | 7.96 |
| CHEMBL4062003 | — | — | 1 | 7.96 |
| CHEMBL4064756 | — | — | 1 | 7.92 |
| CHEMBL4073347 | — | — | 1 | 7.80 |
| CHEMBL4102058 | — | — | 1 | 7.55 |
| CHEMBL4100201 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068509 | PRN-1371 | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4099992 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4089842 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4066763 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4061286 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4088057 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4092456 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4099578 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4095844 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4061766 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4095783 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4081984 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4064081 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4102642 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4083151 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4084708 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4062003 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4064756 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4073347 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4102058 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4100201 | — | IC50 | = | 37.0 | nM | 7.43 |