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Assay Detail

CHEMBL661887

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Binding
Inhibitory activity against human leukocyte cathepsin G (h-CG)
18
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin G (CHEMBL4071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.
Iijima K, Katada J, Hayashi Y.
Bioorg Med Chem Lett (1999) 9 : 413 -418
PubMed 10091694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.91 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108540 1 8.85
CHEMBL335675 1 8.19
CHEMBL134816 1 7.82
CHEMBL436591 2 7.68
CHEMBL424453 1 7.32
CHEMBL134821 2 7.19
CHEMBL134024 1 7.16
CHEMBL131704 1 7.12
CHEMBL135080 1 7.10
CHEMBL338962 1 6.85
CHEMBL134068 1 6.80
CHEMBL134268 1 6.77
CHEMBL336964 1 6.72
CHEMBL131794 1 5.80
CHEMBL134440 1 5.51
CHEMBL131747 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108540 IC50 = 1.4 nM 8.85
CHEMBL335675 IC50 = 6.4 nM 8.19
CHEMBL134816 IC50 = 15.0 nM 7.82
CHEMBL436591 IC50 = 21.0 nM 7.68
CHEMBL424453 IC50 = 48.0 nM 7.32
CHEMBL134821 IC50 = 64.0 nM 7.19
CHEMBL134024 IC50 = 69.0 nM 7.16
CHEMBL131704 IC50 = 75.0 nM 7.12
CHEMBL135080 IC50 = 80.0 nM 7.10
CHEMBL338962 IC50 = 140.0 nM 6.85
CHEMBL134068 IC50 = 160.0 nM 6.80
CHEMBL134268 IC50 = 170.0 nM 6.77
CHEMBL336964 IC50 = 190.0 nM 6.72
CHEMBL134821 IC50 = 250.0 nM 6.60
CHEMBL436591 IC50 = 520.0 nM 6.28
CHEMBL131794 IC50 = 1600.0 nM 5.80
CHEMBL134440 IC50 = 3100.0 nM 5.51
CHEMBL131747 IC50 = 21000.0 nM 4.68