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Compound Detail

CHEMBL5079537

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COc1nc(-c2ncccc2C)cc(-c2ccc(F)cc2)c1C#N

Basic Information

ChEMBL ID CHEMBL5079537
Phase Preclinical
Structure Type MOL
InChI Key PYVOUZRKECXKGO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

319.3
MW (Da)
4.14
ALogP
4
HBA
0
HBD
58.8
PSA (Ų)
0.73
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14FN3O
MW 319.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sulfide:quinone oxidoreductase, mitochondrial
CHEMBL4523512
IC50 8.06 8.06 8.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 42.0 ng.hr.mL-1 Mus musculus
T1/2 5.96 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sulfide:quinone oxidoreductase, mitochondrial IC50 = 8.7 nM 8.06 Inhibition of human SQOR 34763081

Literature References

PubMed DOI Target Context # Activities
34763081 10.1016/j.bmcl.2021.128443 ADMET 5
34763081 10.1016/j.bmcl.2021.128443 Sulfide:quinone oxidoreductase, mitochondrial 1
34763081 10.1016/j.bmcl.2021.128443 No relevant target 1

Data from ChEMBL 36 via Core Engine