Assay Detail
Binding
CHEMBL4013816
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FGFR1 using 5-FAM-KKKKEEIYFFF-NH2 as substrate preincubated for 15 mins followed by peptide substrate addition measured after 3 hrs by caliper capillary electrophoresis method
33
Total Activities
33
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 | 33 | 8.64 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102642 | — | — | 1 | 9.70 |
| CHEMBL4099992 | — | — | 1 | 9.40 |
| CHEMBL4068509 | PRN-1371 | 1.0 | 1 | 9.22 |
| CHEMBL4061766 | — | — | 1 | 9.15 |
| CHEMBL4083740 | — | — | 1 | 9.15 |
| CHEMBL4073347 | — | — | 1 | 9.10 |
| CHEMBL4086567 | — | — | 1 | 9.10 |
| CHEMBL4089842 | — | — | 1 | 9.00 |
| CHEMBL4092456 | — | — | 1 | 9.00 |
| CHEMBL4084708 | — | — | 1 | 8.96 |
| CHEMBL4099578 | — | — | 1 | 8.89 |
| CHEMBL4061286 | — | — | 1 | 8.89 |
| CHEMBL4083151 | — | — | 1 | 8.89 |
| CHEMBL4064081 | — | — | 1 | 8.85 |
| CHEMBL4095844 | — | — | 1 | 8.82 |
| CHEMBL4064756 | — | — | 1 | 8.82 |
| CHEMBL4066763 | — | — | 1 | 8.77 |
| CHEMBL4081984 | — | — | 1 | 8.74 |
| CHEMBL4088057 | — | — | 1 | 8.72 |
| CHEMBL4084079 | — | — | 1 | 8.68 |
| CHEMBL4062003 | — | — | 1 | 8.64 |
| CHEMBL4095783 | — | — | 1 | 8.55 |
| CHEMBL4100201 | — | — | 1 | 8.41 |
| CHEMBL4102058 | — | — | 1 | 8.33 |
| CHEMBL4072676 | — | — | 1 | 8.33 |
| CHEMBL4085605 | — | — | 1 | 8.28 |
| CHEMBL4068712 | — | — | 1 | 8.03 |
| CHEMBL4065128 | — | — | 1 | 7.89 |
| CHEMBL4091839 | — | — | 1 | 7.62 |
| CHEMBL4103536 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102642 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4099992 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4068509 | PRN-1371 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4061766 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4083740 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4073347 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4086567 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4089842 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4092456 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4084708 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4099578 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4061286 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4083151 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4064081 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4064756 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4095844 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4066763 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4081984 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4088057 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4084079 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4062003 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4095783 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4100201 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4102058 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4072676 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4085605 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4068712 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4065128 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4091839 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4103536 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4093349 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4101091 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4065736 | — | IC50 | > | 1000.0 | nM | - |