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Assay Detail

CHEMBL5216080

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

Binding
Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method
6
Total Activities
6
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

Transmembrane protease serine 2 (CHEMBL1795140)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enzyme inhibition as a potential therapeutic strategy to treat COVID-19 infection.
Paulsson-Habegger L, Snabaitis AK, Wren SP.
Bioorg Med Chem (2021) 48 : 116389 -116389
PubMed 34543844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.69 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3219079 1 9.05
CHEMBL3219087 1 9.00
CHEMBL3219102 1 8.52
CHEMBL3219101 1 8.52
CHEMBL3219100 1 8.52
CHEMBL3219103 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3219079 Ki = 0.9 nM 9.05
CHEMBL3219087 Ki = 1.0 nM 9.00
CHEMBL3219102 Ki = 3.0 nM 8.52
CHEMBL3219101 Ki = 3.0 nM 8.52
CHEMBL3219100 Ki = 3.0 nM 8.52
CHEMBL3219103 Ki = 3.0 nM 8.52