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Assay Detail

CHEMBL675303

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

Binding
The compound was tested in vitro for ability to inhibit human leukocyte elastase activity
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.
Warner P, Green RC, Gomes B, Strimpler AM.
J Med Chem (1994) 37 : 3090 -3099
PubMed 7932532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.75 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105233 1 7.92
CHEMBL321296 1 7.50
CHEMBL104303 1 7.47
CHEMBL75936 1 7.44
CHEMBL107291 1 7.40
CHEMBL107191 1 7.38
CHEMBL104289 1 7.33
CHEMBL107966 1 7.32
CHEMBL104032 1 7.29
CHEMBL106793 1 7.16
CHEMBL104557 1 7.15
CHEMBL104396 1 7.06
CHEMBL106066 1 7.06
CHEMBL106888 1 7.05
CHEMBL13684 1 6.55
CHEMBL105124 1 6.50
CHEMBL104050 1 6.46
CHEMBL105067 1 6.30
CHEMBL322177 1 5.58
CHEMBL14223 1 5.57
CHEMBL25490 1 5.55
CHEMBL107329 1 5.47
CHEMBL104250 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105233 Ki = 12.0 nM 7.92
CHEMBL321296 Ki = 32.0 nM 7.50
CHEMBL104303 Ki = 34.0 nM 7.47
CHEMBL75936 Ki = 36.0 nM 7.44
CHEMBL107291 Ki = 40.0 nM 7.40
CHEMBL107191 Ki = 42.0 nM 7.38
CHEMBL104289 Ki = 47.0 nM 7.33
CHEMBL107966 Ki = 48.0 nM 7.32
CHEMBL104032 Ki = 51.0 nM 7.29
CHEMBL106793 Ki = 70.0 nM 7.16
CHEMBL104557 Ki = 71.0 nM 7.15
CHEMBL104396 Ki = 88.0 nM 7.06
CHEMBL106066 Ki = 87.0 nM 7.06
CHEMBL106888 Ki = 89.0 nM 7.05
CHEMBL13684 Ki = 280.0 nM 6.55
CHEMBL105124 Ki = 320.0 nM 6.50
CHEMBL104050 Ki = 350.0 nM 6.46
CHEMBL105067 Ki = 500.0 nM 6.30
CHEMBL322177 Ki = 2600.0 nM 5.58
CHEMBL14223 Ki = 2700.0 nM 5.57
CHEMBL25490 Ki = 2800.0 nM 5.55
CHEMBL107329 Ki = 3400.0 nM 5.47
CHEMBL104250 Ki = 15000.0 nM 4.82