Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to be useful for the treatment of malaria. Twelve organic nitrate derivatives were synthesized and treated with human erythrocyte GR. The molecules were identified as strong GR inhibitors and novel antimalaria candidates. ..more
Target
| Sequence: RecName: Full=Glutathione reductase, mitochondrial; Short=GR; Short=GRase; Flags: Precursor Description ..   Protein Family: Pyridine nucleotide-disulphide oxidoreductase, dimerisation domain Comment .. Gene:GSR Related Protein 3D Structures |
BioActive Compounds: 11
Description:
Title: In vitro inhibition of human erythrocyte glutathione reductase by some new organic nitrates.
Abstract: Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to be useful for the treatment of malaria. Twelve organic nitrate derivatives were synthesized and treated with human erythrocyte GR. The molecules were identified as strong GR inhibitors and novel antimalaria candidates.
(PMID: 19447620)
Abstract: Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to be useful for the treatment of malaria. Twelve organic nitrate derivatives were synthesized and treated with human erythrocyte GR. The molecules were identified as strong GR inhibitors and novel antimalaria candidates.
(PMID: 19447620)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 12642
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 12642
ChEMBL target type: Target is a single protein chain
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | IC50* | IC50 PubChem standard value |  | Float | μM | |
| 2 | IC50 activity comment | IC50 activity comment | String | |||
| 3 | IC50 standard flag | IC50 standard flag | | Integer | ||
| 4 | IC50 qualifier | IC50 qualifier | String | |||
| 5 | IC50 published value | IC50 published value | | Float | nM | |
| 6 | IC50 standard value | IC50 standard value | | Float | nM | |
| 7 | IC50 Binding Efficiency Index(nM) | IC50 Binding Efficiency Index(nM) | | Float | ||
| 8 | Surface Efficiency Index(nM) | Surface Efficiency Index(nM) | | Float | ||
| 9 | Ki activity comment | Ki activity comment | String | |||
| 10 | Ki standard flag | Ki standard flag | | Integer | ||
| 11 | Ki qualifier | Ki qualifier | String | |||
| 12 | Ki published value | Ki published value | | Float | nM | |
| 13 | Ki standard value | Ki standard value | | Float | nM | |
| 14 | Ki Binding Efficiency Index(nM) | Ki Binding Efficiency Index(nM) | | Float | ||
| 15 | Surface Efficiency Index(nM) | Surface Efficiency Index(nM) | | Float |
* Activity Concentration.
Data Table (Concise)
Classification
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