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Assay Detail

CHEMBL677437

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

Binding
Inhibition of human neutrophil elastase-catalyzed hydrolysis of the synthetic substrate MeO-Suc-Ala-Ala-Pro-Val-pNa
33
Total Activities
33
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

Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.
Edwards PD, Zottola MA, Davis M, Williams J, Tuthill PA.
J Med Chem (1995) 38 : 3972 -3982
PubMed 7562931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 9.11 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339307 1 10.22
CHEMBL405664 1 10.00
CHEMBL334978 1 9.74
CHEMBL336779 1 9.70
CHEMBL419985 1 9.70
CHEMBL130966 1 9.52
CHEMBL127714 1 9.48
CHEMBL262516 1 9.47
CHEMBL337931 1 9.46
CHEMBL111029 1 9.43
CHEMBL339650 1 9.37
CHEMBL127615 1 9.30
CHEMBL340818 1 9.30
CHEMBL273818 1 9.26
CHEMBL128499 1 9.22
CHEMBL419800 1 9.19
CHEMBL337968 1 9.18
CHEMBL127780 1 9.18
CHEMBL128553 1 9.09
CHEMBL131580 1 9.00
CHEMBL335233 1 8.96
CHEMBL128415 1 8.96
CHEMBL406200 1 8.89
CHEMBL130002 1 8.82
CHEMBL340627 1 8.74
CHEMBL129496 1 8.72
CHEMBL338651 1 8.64
CHEMBL131107 1 8.62
CHEMBL108783 1 8.52
CHEMBL1237168 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339307 Ki = 0.06 nM 10.22
CHEMBL405664 Ki = 0.1 nM 10.00
CHEMBL334978 Ki = 0.18 nM 9.74
CHEMBL336779 Ki = 0.2 nM 9.70
CHEMBL419985 Ki = 0.2 nM 9.70
CHEMBL130966 Ki = 0.3 nM 9.52
CHEMBL127714 Ki = 0.33 nM 9.48
CHEMBL262516 Ki = 0.34 nM 9.47
CHEMBL337931 Ki = 0.35 nM 9.46
CHEMBL111029 Ki = 0.37 nM 9.43
CHEMBL339650 Ki = 0.43 nM 9.37
CHEMBL127615 Ki = 0.5 nM 9.30
CHEMBL340818 Ki = 0.5 nM 9.30
CHEMBL273818 Ki = 0.55 nM 9.26
CHEMBL128499 Ki = 0.6 nM 9.22
CHEMBL419800 Ki = 0.65 nM 9.19
CHEMBL337968 Ki = 0.66 nM 9.18
CHEMBL127780 Ki = 0.66 nM 9.18
CHEMBL128553 Ki = 0.81 nM 9.09
CHEMBL131580 Ki = 1.0 nM 9.00
CHEMBL335233 Ki = 1.1 nM 8.96
CHEMBL128415 Ki = 1.1 nM 8.96
CHEMBL406200 Ki = 1.3 nM 8.89
CHEMBL130002 Ki = 1.5 nM 8.82
CHEMBL340627 Ki = 1.8 nM 8.74
CHEMBL129496 Ki = 1.9 nM 8.72
CHEMBL338651 Ki = 2.3 nM 8.64
CHEMBL131107 Ki = 2.4 nM 8.62
CHEMBL108783 Ki = 3.0 nM 8.52
CHEMBL1237168 Ki = 4.2 nM 8.38
CHEMBL435413 Ki = 4.4 nM 8.36
CHEMBL336132 Ki = 4.6 nM 8.34
CHEMBL128410 Ki = 11.0 nM 7.96