Assay Detail

CHEMBL5657604

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Binding

Inhibition of human neutrophil elastase using MeOSuc-AAPV-MCA as substrate measured at 60 mins interval for up to several hrs in presence of hydrogen peroxide by fluorescence assay

ChEMBL ↗

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Target

Neutrophil elastase (CHEMBL248) ↗

Open DB target context

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Neutrophil elastase (CHEMBL248) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Neutrophil elastase

CHEMBL248

Anchored from Assay target.

Protein identity Neutrophil elastase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.

von Nussbaum F, Li VM, Allerheiligen S, Anlauf S, Bärfacker L, Bechem M, Delbeck M, Fitzgerald MF, Gerisch M, Gielen-Haertwig H, Haning H, Karthaus D, Lang D, Lustig K, Meibom D, Mittendorf J, Rosentreter U, Schäfer M, Schäfer S, Schamberger J, Telan LA, Tersteegen A.
ChemMedChem (2015) 10 : 1163 -1173
PubMed 26083237 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.85	9.85

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0003818
EFO_TERM	EFO_TERM	-	—	lung disease

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3617973	—	—	1	9.85

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3617973	—	IC50	=	0.14	nM	9.85