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Compound Detail

CHEMBL500504

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Cc1cc(Nc2ccc([N+](=O)[O-])cc2)n2ncnc2n1

Basic Information

ChEMBL ID CHEMBL500504
Phase Preclinical
Structure Type MOL
InChI Key VEPQYHXUPOYESS-UHFFFAOYSA-N

Known Names

DSM-99
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
1
Known Names

Molecular Properties

270.2
MW (Da)
2.08
ALogP
7
HBA
1
HBD
98.2
PSA (Ų)
0.58
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H10N6O2
MW 270.25
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -2.59

Activity Summary

IC50 2 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium berghei
CHEMBL612653
IC50 5.43 5.43 3700.0 1
Dihydroorotate dehydrogenase
CHEMBL3486
IC50 5.37 5.37 4300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium berghei IC50 = 3700.0 nM 5.43 Inhibition of Plasmodium berghei ANKA DHODH 19296651
Dihydroorotate dehydrogenase IC50 = 4300.0 nM 5.37 Inhibition of Plasmodium falciparum DHODH 19296651

Literature References

PubMed DOI Target Context # Activities
19296651 10.1021/jm801343r Plasmodium berghei 1
19296651 10.1021/jm801343r Dihydroorotate dehydrogenase (quinone), mitochondrial 1
19296651 10.1021/jm801343r Plasmodium falciparum 1
19296651 10.1021/jm801343r Dihydroorotate dehydrogenase 1

Data from ChEMBL 36 via Core Engine