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Assay Detail

CHEMBL673106

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Binding
Inhibitory activity against Human Neutrophil Elastase using acute lung injury model (ALIM) assay
ChEMBL ↗
58
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neutrophil elastase (CHEMBL248) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.
Edwards PD, Andisik DW, Bryant CA, Ewing B, Gomes B, Lewis JJ, Rakiewicz D, Steelman G, Strimpler A, Trainor DA, Tuthill PA, Mauger RC, Veale CA, Wildonger RA, Williams JC, Wolanin DJ, Zottola M.
J Med Chem (1997) 40 : 1876 -1885
PubMed 9191965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 8.29 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56136 — — 1 9.39
CHEMBL55912 — — 1 9.37
CHEMBL293809 — — 1 9.30
CHEMBL3085439 — — 1 9.21
CHEMBL2372974 — — 1 9.20
CHEMBL56469 — — 1 9.06
CHEMBL2372979 — — 1 9.02
CHEMBL2372968 — — 1 9.00
CHEMBL56242 — — 1 8.96
CHEMBL56907 — — 1 8.92
CHEMBL293558 — — 1 8.92
CHEMBL417935 — — 2 8.89
CHEMBL301691 — — 1 8.80
CHEMBL354883 — — 1 8.80
CHEMBL542128 — — 1 8.77
CHEMBL55963 — — 1 8.77
CHEMBL418117 — — 1 8.74
CHEMBL56713 — — 1 8.74
CHEMBL55210 — — 2 8.72
CHEMBL2372970 — — 1 8.70
CHEMBL57368 — — 1 8.70
CHEMBL55161 — — 1 8.64
CHEMBL56342 — — 1 8.60
CHEMBL2372969 — — 1 8.59
CHEMBL55726 — — 1 8.57
CHEMBL2372976 — — 1 8.54
CHEMBL55386 — — 1 8.49
CHEMBL54522 — — 1 8.48
CHEMBL2372982 — — 1 8.42
CHEMBL2372966 — — 1 8.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56136 — Ki = 0.41 nM 9.39
CHEMBL55912 — Ki = 0.43 nM 9.37
CHEMBL293809 — Ki = 0.5 nM 9.30
CHEMBL3085439 — Ki = 0.62 nM 9.21
CHEMBL2372974 — Ki = 0.63 nM 9.20
CHEMBL56469 — Ki = 0.87 nM 9.06
CHEMBL2372979 — Ki = 0.96 nM 9.02
CHEMBL2372968 — Ki = 1.0 nM 9.00
CHEMBL56242 — Ki = 1.1 nM 8.96
CHEMBL56907 — Ki = 1.2 nM 8.92
CHEMBL293558 — Ki = 1.2 nM 8.92
CHEMBL417935 — Ki = 1.3 nM 8.89
CHEMBL417935 — Ki = 1.3 nM 8.89
CHEMBL354883 — Ki = 1.6 nM 8.80
CHEMBL301691 — Ki = 1.6 nM 8.80
CHEMBL55963 — Ki = 1.7 nM 8.77
CHEMBL542128 — Ki = 1.7 nM 8.77
CHEMBL418117 — Ki = 1.8 nM 8.74
CHEMBL56713 — Ki = 1.8 nM 8.74
CHEMBL55210 — Ki = 1.9 nM 8.72
CHEMBL55210 — Ki = 1.9 nM 8.72
CHEMBL57368 — Ki = 2.0 nM 8.70
CHEMBL2372970 — Ki = 2.0 nM 8.70
CHEMBL55161 — Ki = 2.3 nM 8.64
CHEMBL56342 — Ki = 2.5 nM 8.60
CHEMBL2372969 — Ki = 2.6 nM 8.59
CHEMBL55726 — Ki = 2.7 nM 8.57
CHEMBL2372976 — Ki = 2.9 nM 8.54
CHEMBL55386 — Ki = 3.2 nM 8.49
CHEMBL54522 — Ki = 3.3 nM 8.48
CHEMBL2372982 — Ki = 3.8 nM 8.42
CHEMBL2372966 — Ki = 3.9 nM 8.41
CHEMBL293707 — Ki = 4.2 nM 8.38
CHEMBL59258 — Ki = 5.2 nM 8.28
CHEMBL292141 — Ki = 5.4 nM 8.27
CHEMBL291309 — Ki = 6.1 nM 8.21
CHEMBL2372965 — Ki = 6.8 nM 8.17
CHEMBL2372977 — Ki = 7.8 nM 8.11
CHEMBL293062 — Ki = 8.0 nM 8.10
CHEMBL435774 — Ki = 10.0 nM 8.00
CHEMBL2372980 — Ki = 11.0 nM 7.96
CHEMBL301825 — Ki = 11.0 nM 7.96
CHEMBL59476 — Ki = 12.0 nM 7.92
CHEMBL2372992 — Ki = 14.0 nM 7.85
CHEMBL2372967 — Ki = 15.0 nM 7.82
CHEMBL56496 — Ki = 15.0 nM 7.82
CHEMBL2372973 — Ki = 16.0 nM 7.80
CHEMBL2372981 — Ki = 20.0 nM 7.70
CHEMBL56852 — Ki = 25.0 nM 7.60
CHEMBL293497 — Ki = 43.0 nM 7.37