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Assay Detail

CHEMBL4307502

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

Binding
Inhibition of human neutrophil elastase using MeOSuc-AAPV-MCA as substrate by fluorescence based assay
3
Total Activities
3
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

Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.
Tian S, Swedberg JE, Li CY, Craik DJ, de Veer SJ.
ACS Med Chem Lett (2019) 10 : 1234 -1239
PubMed 31413811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.97 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557877 1 8.49
CHEMBL4560512 1 7.80
CHEMBL4455694 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557877 Ki = 3.2 nM 8.49
CHEMBL4560512 Ki = 16.0 nM 7.80
CHEMBL4455694 Ki = 24.0 nM 7.62