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Assay Detail

CHEMBL3705545

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

Binding
Inhibition Assay: All the benzisoselenazol-3(2H)-one and bisbenzisoselenazol-3(2H)-one derivatives were tested as potential E. coli TrxR inhibitors by standard DTNB assay.
24
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thioredoxin reductase (CHEMBL3638339)
Type SINGLE PROTEIN
Organism Escherichia coli (strain K12)

Publication

Bacterial thioredoxin reductase inhibitors and methods for use thereof
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.31 5.82
Ki 10 6.64 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035464 2 8.00
CHEMBL2035461 2 7.40
CHEMBL2035460 ETHASELEN 1.0 2 7.30
CHEMBL3655713 2 6.60
CHEMBL3655720 2 6.60
CHEMBL51085 EBSELEN 3.0 2 6.52
CHEMBL3655712 2 6.26
CHEMBL3655716 2 6.00
CHEMBL3655714 2 5.92
CHEMBL3655715 1 5.82
CHEMBL3655721 2 5.82
CHEMBL3655717 1 4.82
CHEMBL3655718 1 4.82
CHEMBL3655719 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035464 Ki = 10.0 nM 8.00
CHEMBL2035461 Ki = 40.0 nM 7.40
CHEMBL2035460 ETHASELEN Ki = 50.0 nM 7.30
CHEMBL3655720 Ki = 250.0 nM 6.60
CHEMBL3655713 Ki = 250.0 nM 6.60
CHEMBL51085 EBSELEN Ki = 300.0 nM 6.52
CHEMBL3655712 Ki = 550.0 nM 6.26
CHEMBL3655716 Ki = 1000.0 nM 6.00
CHEMBL3655714 Ki = 1200.0 nM 5.92
CHEMBL3655721 Ki = 1500.0 nM 5.82
CHEMBL3655715 IC50 = 1500.0 nM 5.82
CHEMBL2035460 ETHASELEN IC50 = 2000.0 nM 5.70
CHEMBL2035461 IC50 = 2100.0 nM 5.68
CHEMBL2035464 IC50 = 2250.0 nM 5.65
CHEMBL3655721 IC50 = 3000.0 nM 5.52
CHEMBL3655720 IC50 = 3000.0 nM 5.52
CHEMBL51085 EBSELEN IC50 = 6000.0 nM 5.22
CHEMBL3655713 IC50 = 6000.0 nM 5.22
CHEMBL3655712 IC50 = 7000.0 nM 5.16
CHEMBL3655714 IC50 = 7500.0 nM 5.12
CHEMBL3655718 IC50 = 15000.0 nM 4.82
CHEMBL3655717 IC50 = 15000.0 nM 4.82
CHEMBL3655716 IC50 = 15000.0 nM 4.82
CHEMBL3655719 IC50 > 40000.0 nM -