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Assay Detail

CHEMBL4307501

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

Binding
Inhibition of purified human proteinase 3 using MeOSuc-AAPV-MCA as substrate by fluorescence based assay
7
Total Activities
7
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

Myeloblastin (CHEMBL3900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.
Tian S, Swedberg JE, Li CY, Craik DJ, de Veer SJ.
ACS Med Chem Lett (2019) 10 : 1234 -1239
PubMed 31413811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.67 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4560512 1 8.21
CHEMBL4557877 1 8.15
CHEMBL4528256 1 8.01
CHEMBL4455694 1 7.77
CHEMBL4589744 1 7.64
CHEMBL4470455 1 7.29
CHEMBL4469546 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4560512 Ki = 6.1 nM 8.21
CHEMBL4557877 Ki = 7.0 nM 8.15
CHEMBL4528256 Ki = 9.8 nM 8.01
CHEMBL4455694 Ki = 17.0 nM 7.77
CHEMBL4589744 Ki = 23.0 nM 7.64
CHEMBL4470455 Ki = 51.0 nM 7.29
CHEMBL4469546 Ki = 245.0 nM 6.61