Assay Detail
Binding
CHEMBL5733863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The compounds were then tested using full-length human recombinant, purified EYA3 and pNPP as a substrate. Compounds were dissolved in DMSO and diluted as needed. IC50 values were determined by adding varying amounts of inhibitor (0-400 μM) to reaction mixtures containing 20 mM MES pH 6, 2 mM MgCl2, 2% DMSO, 3.4 mM pNPP, and 0.01 μg/μL enzyme. Reactions were incubated at 30° C. for 30 minutes and quenched with 100 mM EDTA pH 10. IC50 values were then calculated directly from regression curves using PRISM software. All reported values are the mean of two independent experiments.
9
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Use of small molecule inhibitors targeting EYA tyrosine phosphatase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.89 | 5.00 |
| kon | 3 | - | - |
| k_off | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1523279 | — | — | 3 | 5.00 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 3 | 4.96 |
| CHEMBL1474963 | BENZARONE | 4.0 | 3 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1523279 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1474963 | BENZARONE | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL388590 | BENZBROMARONE | kon | = | - | — | - |
| CHEMBL388590 | BENZBROMARONE | k_off | = | - | s-1 | - |
| CHEMBL1474963 | BENZARONE | kon | = | - | — | - |
| CHEMBL1474963 | BENZARONE | k_off | = | - | s-1 | - |
| CHEMBL1523279 | — | kon | = | - | — | - |
| CHEMBL1523279 | — | k_off | = | - | s-1 | - |