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Assay Detail

CHEMBL698901

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

Binding
Inhibition of Human Leukocyte Elastase (HLE) as apparent binding constant (kreact/kinact)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastase
Desai RC, Dunlap RP, Farrell RP, Ferguson E, Franke CA, Gordon R, Hlasta DJ, Talomie TG
Bioorg Med Chem Lett (1995) 5 : 105 -109
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 9.75 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12082 1 10.66
CHEMBL11558 1 10.31
CHEMBL430157 1 10.15
CHEMBL12051 1 10.10
CHEMBL11874 1 10.10
CHEMBL269223 1 9.96
CHEMBL11758 1 9.77
CHEMBL11913 1 9.62
CHEMBL274582 1 9.47
CHEMBL274347 1 9.33
CHEMBL416154 1 8.92
CHEMBL274085 1 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12082 Ki = 0.022 nM 10.66
CHEMBL11558 Ki = 0.049 nM 10.31
CHEMBL430157 Ki = 0.07 nM 10.15
CHEMBL12051 Ki = 0.08 nM 10.10
CHEMBL11874 Ki = 0.08 nM 10.10
CHEMBL269223 Ki = 0.11 nM 9.96
CHEMBL11758 Ki = 0.17 nM 9.77
CHEMBL11913 Ki = 0.24 nM 9.62
CHEMBL274582 Ki = 0.34 nM 9.47
CHEMBL274347 Ki = 0.47 nM 9.33
CHEMBL416154 Ki = 1.2 nM 8.92
CHEMBL274085 Ki = 2.7 nM 8.57