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Assay Detail

CHEMBL677607

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

Binding
In vitro inhibition constant (Ki) against human leukocyte elastase (HLE-catalyzed hydrolysis of MeO-Suc-Ala-Ala-Pro-Ala-pNA)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.
Bernstein PR, Gomes BC, Kosmider BJ, Vacek EP, Williams JC.
J Med Chem (1995) 38 : 212 -215
PubMed 7837235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.99 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307315 1 9.15
CHEMBL55210 1 8.72
CHEMBL304354 1 8.22
CHEMBL66579 1 8.10
CHEMBL303165 1 8.08
CHEMBL303493 1 8.03
CHEMBL308881 1 7.75
CHEMBL66520 1 7.58
CHEMBL68841 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307315 Ki = 0.7 nM 9.15
CHEMBL55210 Ki = 1.9 nM 8.72
CHEMBL304354 Ki = 6.0 nM 8.22
CHEMBL66579 Ki = 8.0 nM 8.10
CHEMBL303165 Ki = 8.4 nM 8.08
CHEMBL303493 Ki = 9.4 nM 8.03
CHEMBL308881 Ki = 18.0 nM 7.75
CHEMBL66520 Ki = 26.0 nM 7.58
CHEMBL68841 Ki = 480.0 nM 6.32