Assay Detail
Binding
CHEMBL5239773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FGFR4 V550L (unknown origin) using TK as substrate incubated for 1 hr in presence of biotin/ATP by HTRF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.80 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | 1.0 | 1 | 9.10 |
| CHEMBL5283096 | — | — | 1 | 7.75 |
| CHEMBL5290554 | — | — | 1 | 7.61 |
| CHEMBL5278656 | — | — | 1 | 7.51 |
| CHEMBL5281307 | — | — | 1 | 7.45 |
| CHEMBL5289886 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828009 | LY-2874455 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5283096 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5290554 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL5278656 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL5281307 | — | IC50 | = | 35.2 | nM | 7.45 |
| CHEMBL5289886 | — | IC50 | = | 43.5 | nM | 7.36 |