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Assay Detail

CHEMBL676742

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

Binding
Tested for inhibitory activity against human leukocyte elastase(HLE) enzyme
20
Total Activities
20
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

Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones.
Damewood JR, Edwards PD, Feeney S, Gomes BC, Steelman GB, Tuthill PA, Williams JC, Warner P, Woolson SA, Wolanin DJ.
J Med Chem (1994) 37 : 3303 -3312
PubMed 7932558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.58 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325234 1 8.46
CHEMBL112880 1 8.42
CHEMBL113132 1 8.36
CHEMBL11391 1 8.35
CHEMBL113321 1 8.25
CHEMBL113261 1 8.18
CHEMBL113171 1 8.07
CHEMBL418822 1 8.04
CHEMBL432961 1 7.96
CHEMBL432442 1 7.51
CHEMBL325873 1 7.50
CHEMBL326616 1 7.48
CHEMBL107291 1 7.40
CHEMBL322360 1 7.38
CHEMBL112971 1 7.18
CHEMBL109852 1 7.10
CHEMBL13684 1 6.55
CHEMBL114024 1 6.52
CHEMBL324587 1 6.50
CHEMBL109769 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325234 Ki = 3.5 nM 8.46
CHEMBL112880 Ki = 3.8 nM 8.42
CHEMBL113132 Ki = 4.4 nM 8.36
CHEMBL11391 Ki = 4.5 nM 8.35
CHEMBL113321 Ki = 5.6 nM 8.25
CHEMBL113261 Ki = 6.6 nM 8.18
CHEMBL113171 Ki = 8.5 nM 8.07
CHEMBL418822 Ki = 9.1 nM 8.04
CHEMBL432961 Ki = 11.0 nM 7.96
CHEMBL432442 Ki = 31.0 nM 7.51
CHEMBL325873 Ki = 32.0 nM 7.50
CHEMBL326616 Ki = 33.0 nM 7.48
CHEMBL107291 Ki = 40.0 nM 7.40
CHEMBL322360 Ki = 42.0 nM 7.38
CHEMBL112971 Ki = 66.0 nM 7.18
CHEMBL109852 Ki = 79.0 nM 7.10
CHEMBL13684 Ki = 280.0 nM 6.55
CHEMBL114024 Ki = 300.0 nM 6.52
CHEMBL324587 Ki = 320.0 nM 6.50
CHEMBL109769 Ki = 360.0 nM 6.44