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Assay Detail

CHEMBL5657600

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

Binding
Competitive inhibition of human neutrophil elastase using varying levels of MeOSuc-AAPV-MCA as substrate measured at 60 mins interval for up to several hrs by Dixon plot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
2
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
Ki 2 8.96 10.10

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 10.10
CHEMBL3617968 BAY-678 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617973 Ki = 0.08 nM 10.10
CHEMBL3617968 BAY-678 Ki = 15.0 nM 7.82