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Compound Detail

CHEMBL575013

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N#Cc1c(-c2cccc(-c3no[n+]([O-])c3C#N)c2)no[n+]1[O-]

Basic Information

ChEMBL ID CHEMBL575013
Phase Preclinical
Structure Type MOL
InChI Key SMSDDAFMMQEAII-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

296.2
MW (Da)
0.01
ALogP
8
HBA
0
HBD
153.5
PSA (Ų)
0.60
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H4N6O4
MW 296.20
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.76

Activity Summary

IC50 2 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thioredoxin glutathione reductase
CHEMBL6110
IC50 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thioredoxin glutathione reductase IC50 = 3500.0 nM 5.46 Inhibition of Schistosoma mansoni TGR 19761212

Literature References

PubMed DOI Target Context # Activities
19761212 10.1021/jm901021k Schistosoma mansoni 6
19761212 10.1021/jm901021k No relevant target 2
19761212 10.1021/jm901021k Thioredoxin glutathione reductase 2
19761212 10.1021/jm901021k Caco-2 2
19761212 10.1021/jm901021k Thioredoxin reductase 1, cytoplasmic 1
19761212 10.1021/jm901021k Glutathione reductase, mitochondrial 1
19761212 10.1021/jm901021k Liver microsomes 1
19761212 10.1021/jm901021k Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine