Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL677601

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-p- nitroanilide.
39
Total Activities
37
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

Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones.
Edwards PD, Andisik DW, Strimpler AM, Gomes B, Tuthill PA.
J Med Chem (1996) 39 : 1112 -1124
PubMed 8676347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 7.34 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276307 1 9.02
CHEMBL354883 1 8.80
CHEMBL13753 1 8.55
CHEMBL11391 2 8.35
CHEMBL14121 1 8.24
CHEMBL14165 1 8.12
CHEMBL275043 1 8.10
CHEMBL14293 1 8.08
CHEMBL275340 1 8.00
CHEMBL14115 1 8.00
CHEMBL13902 1 7.92
CHEMBL13954 1 7.82
CHEMBL13863 1 7.82
CHEMBL14631 1 7.80
CHEMBL278222 1 7.80
CHEMBL278912 1 7.72
CHEMBL273486 1 7.68
CHEMBL268005 1 7.66
CHEMBL14177 1 7.58
CHEMBL14064 1 7.38
CHEMBL13740 1 7.36
CHEMBL13923 1 7.21
CHEMBL14222 1 7.13
CHEMBL416159 1 7.00
CHEMBL13937 1 6.80
CHEMBL276181 1 6.64
CHEMBL13684 2 6.55
CHEMBL14176 1 6.54
CHEMBL13804 1 6.51
CHEMBL269448 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276307 Ki = 0.95 nM 9.02
CHEMBL354883 Ki = 1.6 nM 8.80
CHEMBL13753 Ki = 2.8 nM 8.55
CHEMBL11391 Ki = 4.5 nM 8.35
CHEMBL11391 Ki = 4.5 nM 8.35
CHEMBL14121 Ki = 5.7 nM 8.24
CHEMBL14165 Ki = 7.5 nM 8.12
CHEMBL275043 Ki = 8.0 nM 8.10
CHEMBL14293 Ki = 8.4 nM 8.08
CHEMBL14115 Ki = 10.0 nM 8.00
CHEMBL275340 Ki = 9.9 nM 8.00
CHEMBL13902 Ki = 12.0 nM 7.92
CHEMBL13863 Ki = 15.0 nM 7.82
CHEMBL13954 Ki = 15.0 nM 7.82
CHEMBL14631 Ki = 16.0 nM 7.80
CHEMBL278222 Ki = 16.0 nM 7.80
CHEMBL278912 Ki = 19.0 nM 7.72
CHEMBL273486 Ki = 21.0 nM 7.68
CHEMBL268005 Ki = 22.0 nM 7.66
CHEMBL14177 Ki = 26.0 nM 7.58
CHEMBL14064 Ki = 42.0 nM 7.38
CHEMBL13740 Ki = 44.0 nM 7.36
CHEMBL13923 Ki = 62.0 nM 7.21
CHEMBL14222 Ki = 74.0 nM 7.13
CHEMBL416159 Ki = 100.0 nM 7.00
CHEMBL13937 Ki = 160.0 nM 6.80
CHEMBL276181 Ki = 230.0 nM 6.64
CHEMBL13684 Ki = 280.0 nM 6.55
CHEMBL13684 Ki = 280.0 nM 6.55
CHEMBL14176 Ki = 290.0 nM 6.54
CHEMBL13804 Ki = 310.0 nM 6.51
CHEMBL269448 Ki = 330.0 nM 6.48
CHEMBL14516 Ki = 469.0 nM 6.33
CHEMBL14128 Ki = 490.0 nM 6.31
CHEMBL267800 Ki = 620.0 nM 6.21
CHEMBL273612 Ki = 690.0 nM 6.16
CHEMBL276182 Ki = 830.0 nM 6.08
CHEMBL275723 Ki = 910.0 nM 6.04
CHEMBL14223 Ki = 2700.0 nM 5.57