Assay Detail
Binding
CHEMBL3706367
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Release Assay: Each of Compounds (1) to (6) was dissolved in 100% DMSO so as to obtain stock to compound solutions with concentrations of 0.01, 0.03, 0.1, 0.3, 1, 3 or 10 mM) for each of Compounds (1) to (6). 7500 of the neutrophil suspension obtained in -3. Preparation of human neutrophil under the section of -Experimental materials was added with 200 uM of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide (454454, Calbiochem Limited, dissolved in 750 ul HBSS and functioned as a substrate for human neutrophils) at a is volume ratio of 1:1 (the final volume was 1.5 ml), stirred at 37 C. for 2 minutes, followed by addition with 1.5 ul of the aforesaid compound solution and reaction at 37 C. for 2 minutes. In a control group, 100% DMSO was used to substitute the compound solution. Moreover, Sivelestat (with concentrations of 0.01, 0.03, 0.1, 0.3, 1, 3 or 10 mM in DMSO) was used to substitute the compound solution as a positive control group.
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
Oxime-based compound, pharmaceutical composition containing the same and method for preparing the same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.04 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3697032 | — | — | 1 | 7.52 |
| CHEMBL76688 | SIVELESTAT | 3.0 | 1 | 7.30 |
| CHEMBL3697035 | — | — | 1 | 7.10 |
| CHEMBL3697033 | — | — | 1 | 6.96 |
| CHEMBL3697034 | — | — | 1 | 6.89 |
| CHEMBL3398151 | — | — | 1 | 6.77 |
| CHEMBL3398152 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3697032 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL76688 | SIVELESTAT | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3697035 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3697033 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3697034 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3398151 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3398152 | — | IC50 | = | 180.0 | nM | 6.75 |