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Assay Detail

CHEMBL4380412

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

Binding
Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs
11
Total Activities
11
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

Cathepsin G (CHEMBL4071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.
Li CY, Yap K, Swedberg JE, Craik DJ, de Veer SJ.
J Med Chem (2020) 63 : 816 -826
PubMed 31855419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.31 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4592765 1 9.59
CHEMBL4469390 1 8.13
CHEMBL4586444 1 8.09
CHEMBL4590739 1 7.85
CHEMBL4457132 1 7.27
CHEMBL4560112 1 6.82
CHEMBL4465306 1 6.80
CHEMBL4554739 1 5.92
CHEMBL4556207 1 5.28
CHEMBL4450993 1 -
CHEMBL4472737 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4592765 Ki = 0.26 nM 9.59
CHEMBL4469390 Ki = 7.4 nM 8.13
CHEMBL4586444 Ki = 8.2 nM 8.09
CHEMBL4590739 Ki = 14.0 nM 7.85
CHEMBL4457132 Ki = 54.0 nM 7.27
CHEMBL4560112 Ki = 150.0 nM 6.82
CHEMBL4465306 Ki = 160.0 nM 6.80
CHEMBL4554739 Ki = 1200.0 nM 5.92
CHEMBL4556207 Ki = 5200.0 nM 5.28
CHEMBL4450993 Ki < 0.1 nM -
CHEMBL4472737 Ki - -