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Assay Detail

CHEMBL932239

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

Binding
Inhibition of human neutrophil elastase
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Maryanoff BE, Costanzo MJ.
Bioorg Med Chem (2008) 16 : 1562 -1595
PubMed 18053726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 8.02 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285231 1 10.60
CHEMBL403098 1 10.22
CHEMBL334978 1 10.00
CHEMBL270680 1 9.70
CHEMBL336779 1 9.70
CHEMBL127714 1 9.48
CHEMBL262516 1 9.47
CHEMBL404910 1 9.46
CHEMBL24058 1 9.31
CHEMBL277672 1 9.28
CHEMBL354832 1 9.22
CHEMBL283168 1 9.19
CHEMBL256466 1 9.18
CHEMBL404871 1 9.09
CHEMBL406200 1 8.89
CHEMBL278134 1 8.85
CHEMBL354883 1 8.80
CHEMBL338651 1 8.64
CHEMBL108783 1 8.52
CHEMBL23234 1 8.44
CHEMBL270651 1 8.19
CHEMBL282705 1 8.19
CHEMBL128410 1 7.96
CHEMBL25892 FRESELESTAT 2.0 1 7.92
CHEMBL353441 1 7.60
CHEMBL352305 1 7.55
CHEMBL165525 1 7.39
CHEMBL438709 1 7.14
CHEMBL169842 1 6.57
CHEMBL167824 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285231 Ki = 0.025 nM 10.60
CHEMBL403098 Ki = 0.06 nM 10.22
CHEMBL334978 Ki = 0.1 nM 10.00
CHEMBL270680 Ki = 0.2 nM 9.70
CHEMBL336779 Ki = 0.2 nM 9.70
CHEMBL127714 Ki = 0.33 nM 9.48
CHEMBL262516 Ki = 0.34 nM 9.47
CHEMBL404910 Ki = 0.35 nM 9.46
CHEMBL24058 Ki = 0.49 nM 9.31
CHEMBL277672 Ki = 0.52 nM 9.28
CHEMBL354832 Ki = 0.6 nM 9.22
CHEMBL283168 Ki = 0.64 nM 9.19
CHEMBL256466 Ki = 0.66 nM 9.18
CHEMBL404871 Ki = 0.81 nM 9.09
CHEMBL406200 Ki = 1.3 nM 8.89
CHEMBL278134 Ki = 1.4 nM 8.85
CHEMBL354883 Ki = 1.6 nM 8.80
CHEMBL338651 Ki = 2.3 nM 8.64
CHEMBL108783 Ki = 3.0 nM 8.52
CHEMBL23234 Ki = 3.6 nM 8.44
CHEMBL270651 Ki = 6.4 nM 8.19
CHEMBL282705 Ki = 6.4 nM 8.19
CHEMBL128410 Ki = 11.0 nM 7.96
CHEMBL25892 FRESELESTAT Ki = 12.0 nM 7.92
CHEMBL353441 Ki = 25.0 nM 7.60
CHEMBL352305 Ki = 28.0 nM 7.55
CHEMBL165525 Ki = 41.0 nM 7.39
CHEMBL438709 Ki = 73.0 nM 7.14
CHEMBL169842 Ki = 270.0 nM 6.57
CHEMBL167824 Ki = 3400.0 nM 5.47
CHEMBL168761 Ki = 5600.0 nM 5.25
CHEMBL355477 Ki = 8000.0 nM 5.10
CHEMBL169076 Ki = 12000.0 nM 4.92
CHEMBL257889 Ki = 21000.0 nM 4.68
CHEMBL168834 Ki = 22000.0 nM 4.66
CHEMBL169750 Ki = 80000.0 nM 4.10