Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3706367

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Oxime-based compound, pharmaceutical composition containing the same and method for preparing the same
(2015)

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