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Assay Detail

CHEMBL2319792

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

Binding
Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T84
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thioredoxin (CHEMBL2010624)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibition of extracellular thioredoxin by asymmetric disulfides.
DiRaimondo TR, Plugis NM, Jin X, Khosla C.
J Med Chem (2013) 56 : 1301 -1310
PubMed 23327656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.32 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2315295 1 7.05
CHEMBL2315297 1 6.77
CHEMBL2315294 1 6.62
CHEMBL2315292 1 6.54
CHEMBL2315306 1 6.47
CHEMBL2315290 1 6.35
CHEMBL2315299 1 6.29
CHEMBL2315288 1 6.27
CHEMBL406050 PX-12 2.0 1 5.68
CHEMBL2315305 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2315295 IC50 = 90.0 nM 7.05
CHEMBL2315297 IC50 = 170.0 nM 6.77
CHEMBL2315294 IC50 = 240.0 nM 6.62
CHEMBL2315292 IC50 = 290.0 nM 6.54
CHEMBL2315306 IC50 = 340.0 nM 6.47
CHEMBL2315290 IC50 = 450.0 nM 6.35
CHEMBL2315299 IC50 = 510.0 nM 6.29
CHEMBL2315288 IC50 = 540.0 nM 6.27
CHEMBL406050 PX-12 IC50 = 2110.0 nM 5.68
CHEMBL2315305 IC50 = 7310.0 nM 5.14