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Compound Detail

CHEMBL170303

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CC(C)COc1ccc(-n2cc(C(=O)O)cn2)cc1C#N

Basic Information

ChEMBL ID CHEMBL170303
Phase Preclinical
Structure Type MOL
InChI Key ARVOJZNLBNQCMK-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
12
PK Parameters
3
Publications
0
Known Names

Molecular Properties

285.3
MW (Da)
2.48
ALogP
5
HBA
1
HBD
88.1
PSA (Ų)
0.91
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N3O3
MW 285.30
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -1.78

Activity Summary

IC50 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Xanthine dehydrogenase/oxidase
CHEMBL3649
IC50 8.15 8.15 7.1 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 410.0 ng.hr.mL-1 Rattus norvegicus
AUC 3560.0 ng.hr.mL-1 Rattus norvegicus
AUC 650.0 ng.hr.mL-1 Rattus norvegicus
AUC 5380.0 ng.hr.mL-1 Rattus norvegicus
AUC 620.0 ng.hr.mL-1 Rattus norvegicus
AUC 5160.0 ng.hr.mL-1 Rattus norvegicus
Cmax 315.46 nM Rattus norvegicus
Cmax 4065.9 nM Rattus norvegicus
T1/2 3.3 hr Rattus norvegicus
T1/2 3.5 hr Rattus norvegicus
Tmax 1.1 hr Rattus norvegicus
Tmax 1.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11294382 10.1016/s0960-894x(01)00093-2 Rattus norvegicus 15
28478180 10.1016/j.ejmech.2017.04.031 Xanthine dehydrogenase/oxidase 2
11294382 10.1016/s0960-894x(01)00093-2 Xanthine dehydrogenase/oxidase 1

Data from ChEMBL 36 via Core Engine