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Assay Detail

CHEMBL699807

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

Binding
Inhibition of human neutrophil elastase HNE, hydrolysis of MeO-Suc-Ala-Ala-Pro-Val-pNa
14
Total Activities
14
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 and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.
Ohmoto K, Yamamoto T, Horiuchi T, Imanishi H, Odagaki Y, Kawabata K, Sekioka T, Hirota Y, Matsuoka S, Nakai H, Toda M, Cheronis JC, Spruce LW, Gyorkos A, Wieczorek M.
J Med Chem (2000) 43 : 4927 -4929
PubMed 11150162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.46 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285231 1 10.60
CHEMBL24058 1 9.31
CHEMBL277672 1 9.28
CHEMBL283168 1 9.19
CHEMBL279941 1 8.93
CHEMBL278134 1 8.86
CHEMBL23234 1 8.45
CHEMBL282705 1 8.20
CHEMBL26499 1 7.93
CHEMBL25892 FRESELESTAT 2.0 1 7.92
CHEMBL277401 1 7.82
CHEMBL147676 1 7.54
CHEMBL22927 1 7.35
CHEMBL428848 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285231 Ki = 0.025 nM 10.60
CHEMBL24058 Ki = 0.49 nM 9.31
CHEMBL277672 Ki = 0.52 nM 9.28
CHEMBL283168 Ki = 0.64 nM 9.19
CHEMBL279941 Ki = 1.18 nM 8.93
CHEMBL278134 Ki = 1.37 nM 8.86
CHEMBL23234 Ki = 3.59 nM 8.45
CHEMBL282705 Ki = 6.38 nM 8.20
CHEMBL26499 Ki = 11.8 nM 7.93
CHEMBL25892 FRESELESTAT Ki = 12.16 nM 7.92
CHEMBL277401 Ki = 15.3 nM 7.82
CHEMBL147676 Ki = 29.1 nM 7.54
CHEMBL22927 Ki = 44.3 nM 7.35
CHEMBL428848 Ki = 101.0 nM 7.00