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Assay Detail

CHEMBL5506181

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

Binding
Inhibition of human TMPRSS2
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

Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors.
Wu A, Shi K, Wang J, Zhang R, Wang Y.
Eur J Med Chem (2024) 263 : 115923 -115923
PubMed 37981443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.31 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273264 NAFAMOSTAT 3.0 1 9.30
CHEMBL590799 CAMOSTAT 3.0 1 8.41
CHEMBL1185793 1 7.16
CHEMBL87563 GABEXATE 3.0 1 6.89
CHEMBL46618 OTAMIXABAN 3.0 1 6.21
CHEMBL147503 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273264 NAFAMOSTAT IC50 = 0.5 nM 9.30
CHEMBL590799 CAMOSTAT IC50 = 3.9 nM 8.41
CHEMBL1185793 IC50 = 70.0 nM 7.16
CHEMBL87563 GABEXATE IC50 = 130.0 nM 6.89
CHEMBL46618 OTAMIXABAN IC50 = 620.0 nM 6.21
CHEMBL147503 IC50 = 1240.0 nM 5.91