Assay Detail
Binding
CHEMBL3705672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time-Resolved Fluorescence Assay: The following assay may be used to determine the activity of the compounds of the invention for inhibiting EGFR kinase activity. The half maximal inhibitory concentration IC50 (the concentration of the tested compound showing 50% inhibition of the enzyme activity) of each compound was determined by incubating several different concentrations of the tested compounds with a specific enzyme and substrate. EGFR kinase used in this assay is a human-derived recombinant protein (Cell signaling technology, #7908), which was reacted with peptide substrate and different concentrations of tested compounds in a buffer solution containing 60 mM HEPES (pH7.5), 5 mM MgCl2, 5 mM MnCl2, 3 μM Na3VO4, 1.25 M DTT (1000×) and 20 μM ATP at 25° C., for 45 minutes.
7
Total Activities
7
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
6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.07 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3647422 | — | — | 1 | 8.70 |
| CHEMBL3647423 | — | — | 1 | 8.70 |
| CHEMBL3647421 | — | — | 1 | 8.40 |
| CHEMBL3647418 | — | — | 1 | 8.22 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 7.89 |
| CHEMBL3647417 | — | — | 1 | 7.32 |
| CHEMBL3647419 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3647422 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647423 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647421 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3647418 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3647417 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3647419 | — | IC50 | = | 59.0 | nM | 7.23 |