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Assay Detail

CHEMBL2208690

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

Binding
Inhibition of human neutrophil elastase
18
Total Activities
18
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

Synopsis of some recent tactical application of bioisosteres in drug design.
Meanwell NA.
J Med Chem (2011) 54 : 2529 -2591
PubMed 21413808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.66 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285231 1 10.60
CHEMBL24058 1 9.31
CHEMBL2205678 1 9.22
CHEMBL354883 1 8.80
CHEMBL108783 1 8.52
CHEMBL353441 1 7.60
CHEMBL352305 1 7.55
CHEMBL165525 1 7.39
CHEMBL169842 1 6.57
CHEMBL167824 1 5.47
CHEMBL168120 1 5.37
CHEMBL168761 1 5.25
CHEMBL355477 1 5.10
CHEMBL169076 1 4.92
CHEMBL355765 1 4.80
CHEMBL166859 1 4.68
CHEMBL168834 1 4.66
CHEMBL169750 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285231 Ki = 0.025 nM 10.60
CHEMBL24058 Ki = 0.49 nM 9.31
CHEMBL2205678 Ki = 0.6 nM 9.22
CHEMBL354883 Ki = 1.6 nM 8.80
CHEMBL108783 Ki = 3.0 nM 8.52
CHEMBL353441 Ki = 25.0 nM 7.60
CHEMBL352305 Ki = 28.0 nM 7.55
CHEMBL165525 Ki = 41.0 nM 7.39
CHEMBL169842 Ki = 270.0 nM 6.57
CHEMBL167824 Ki = 3400.0 nM 5.47
CHEMBL168120 Ki = 4300.0 nM 5.37
CHEMBL168761 Ki = 5600.0 nM 5.25
CHEMBL355477 Ki = 8000.0 nM 5.10
CHEMBL169076 Ki = 12000.0 nM 4.92
CHEMBL355765 Ki = 16000.0 nM 4.80
CHEMBL166859 Ki = 21000.0 nM 4.68
CHEMBL168834 Ki = 22000.0 nM 4.66
CHEMBL169750 Ki = 80000.0 nM 4.10