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Assay Detail

CHEMBL673105

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Binding
Inhibition of Human Leukocyte Elastase (HLE)
13
Total Activities
13
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

Design of orally active, non-peptidic inhibitors of human leukocyte elastase.
Brown FJ, Andisik DW, Bernstein PR, Bryant CB, Ceccarelli C, Damewood JR, Edwards PD, Earley RA, Feeney S, Green RC.
J Med Chem (1994) 37 : 1259 -1261
PubMed 8176703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.77 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276307 1 9.03
CHEMBL282694 1 8.74
CHEMBL11391 1 8.35
CHEMBL280916 1 8.24
CHEMBL11403 1 8.18
CHEMBL275043 1 8.10
CHEMBL11098 1 8.09
CHEMBL277905 1 7.89
CHEMBL279250 1 7.75
CHEMBL11336 1 7.40
CHEMBL428848 1 7.00
CHEMBL2371666 1 6.68
CHEMBL25490 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276307 Ki = 0.93 nM 9.03
CHEMBL282694 Ki = 1.8 nM 8.74
CHEMBL11391 Ki = 4.5 nM 8.35
CHEMBL280916 Ki = 5.7 nM 8.24
CHEMBL11403 Ki = 6.6 nM 8.18
CHEMBL275043 Ki = 8.0 nM 8.10
CHEMBL11098 Ki = 8.2 nM 8.09
CHEMBL277905 Ki = 13.0 nM 7.89
CHEMBL279250 Ki = 18.0 nM 7.75
CHEMBL11336 Ki = 40.0 nM 7.40
CHEMBL428848 Ki = 101.0 nM 7.00
CHEMBL2371666 Ki = 210.0 nM 6.68
CHEMBL25490 Ki = 2800.0 nM 5.55