Assay Detail
Binding
CHEMBL4833162
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay
39
Total Activities
39
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
Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.87 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4866267 | — | — | 1 | 9.26 |
| CHEMBL4866362 | — | — | 1 | 9.00 |
| CHEMBL4856555 | — | — | 1 | 9.00 |
| CHEMBL4848448 | — | — | 1 | 8.96 |
| CHEMBL4864145 | — | — | 1 | 8.96 |
| CHEMBL4847845 | — | — | 1 | 8.77 |
| CHEMBL4852633 | — | — | 1 | 8.74 |
| CHEMBL4869676 | — | — | 1 | 8.72 |
| CHEMBL4855941 | — | — | 1 | 8.70 |
| CHEMBL4869377 | — | — | 1 | 8.59 |
| CHEMBL4859949 | — | — | 1 | 8.49 |
| CHEMBL4870186 | — | — | 1 | 8.49 |
| CHEMBL4865511 | — | — | 1 | 8.44 |
| CHEMBL4877860 | — | — | 1 | 8.44 |
| CHEMBL4858227 | — | — | 1 | 8.26 |
| CHEMBL4852405 | — | — | 1 | 8.26 |
| CHEMBL4849814 | — | — | 1 | 8.24 |
| CHEMBL4859584 | — | — | 1 | 8.11 |
| CHEMBL4871076 | — | — | 1 | 8.07 |
| CHEMBL4872856 | — | — | 1 | 8.07 |
| CHEMBL4849516 | — | — | 1 | 8.00 |
| CHEMBL4862742 | — | — | 1 | 8.00 |
| CHEMBL4854826 | — | — | 1 | 7.96 |
| CHEMBL4868698 | — | — | 1 | 7.89 |
| CHEMBL4068896 | — | — | 1 | 7.85 |
| CHEMBL4856720 | — | — | 1 | 7.85 |
| CHEMBL4864326 | — | — | 1 | 7.77 |
| CHEMBL4879303 | — | — | 1 | 7.52 |
| CHEMBL4860524 | — | — | 1 | 7.51 |
| CHEMBL4877857 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4866267 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL4866362 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4856555 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4848448 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4864145 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4847845 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4852633 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4869676 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4855941 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4869377 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4859949 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4870186 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4865511 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4877860 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4852405 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4858227 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4849814 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4859584 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4872856 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4871076 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4849516 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4862742 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4854826 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4868698 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4068896 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4856720 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4864326 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4879303 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4860524 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4877857 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4848790 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4872134 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4858689 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4852693 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL4852691 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4849580 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL4874552 | — | IC50 | = | 986.0 | nM | 6.01 |
| CHEMBL4872953 | — | IC50 | = | 3577.0 | nM | 5.45 |
| CHEMBL4871039 | — | IC50 | = | 4011.0 | nM | 5.40 |