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Assay Detail

CHEMBL897087

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Binding
Inhibition of human GR
13
Total Activities
13
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

Glutathione reductase, mitochondrial (CHEMBL2755)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity.
Martyn DC, Jones DC, Fairlamb AH, Clardy J.
Bioorg Med Chem Lett (2007) 17 : 1280 -1283
PubMed 17197182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.37 4.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535173 1 4.69
CHEMBL537483 1 4.69
CHEMBL538585 1 4.60
CHEMBL233347 1 4.24
CHEMBL536752 1 4.19
CHEMBL55756 1 4.10
CHEMBL233348 1 4.06
CHEMBL231735 1 -
CHEMBL234180 1 -
CHEMBL395223 1 -
CHEMBL233549 1 -
CHEMBL233339 1 -
CHEMBL392238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535173 IC50 = 20400.0 nM 4.69
CHEMBL537483 IC50 = 20300.0 nM 4.69
CHEMBL538585 IC50 = 24900.0 nM 4.60
CHEMBL233347 IC50 = 58000.0 nM 4.24
CHEMBL536752 IC50 = 64800.0 nM 4.19
CHEMBL55756 IC50 = 79300.0 nM 4.10
CHEMBL233348 IC50 = 86300.0 nM 4.06
CHEMBL231735 IC50 > 157000.0 nM -
CHEMBL234180 IC50 > 212000.0 nM -
CHEMBL395223 IC50 > 155000.0 nM -
CHEMBL233549 IC50 > 173000.0 nM -
CHEMBL233339 IC50 > 135000.0 nM -
CHEMBL392238 IC50 = 105000.0 nM -