Assay Detail
Binding
CHEMBL4714828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged FGFR4 (781 to 1338 residues) cytoplasmic domain expressed in baculovirus expression system using Tyr 04 peptide as substrate incubated for 1 hr in presence of ATP by Z'-LYTE assay
12
Total Activities
12
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
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.99 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3908979 | FGF401 | 2.0 | 1 | 8.00 |
| CHEMBL4742889 | — | — | 1 | 7.80 |
| CHEMBL4757810 | — | — | 1 | 7.35 |
| CHEMBL4785949 | — | — | 1 | 7.28 |
| CHEMBL4061083 | — | — | 1 | 7.14 |
| CHEMBL4740775 | — | — | 1 | 6.17 |
| CHEMBL4763652 | — | — | 1 | 5.21 |
| CHEMBL4750816 | — | — | 1 | - |
| CHEMBL4748301 | — | — | 1 | - |
| CHEMBL4739914 | — | — | 1 | - |
| CHEMBL4799486 | — | — | 1 | - |
| CHEMBL4796512 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3908979 | FGF401 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4742889 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4757810 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4785949 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4061083 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4740775 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4763652 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4750816 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4748301 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4739914 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4799486 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4796512 | — | IC50 | > | 10000.0 | nM | - |