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Compound Detail

CHEMBL461228

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COCCOCOc1ccc(-c2nc(-c3ccnc(C)c3)n[nH]2)cc1C#N

Basic Information

ChEMBL ID CHEMBL461228
Phase Preclinical
Structure Type MOL
InChI Key WABKDMUUPNILOR-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

365.4
MW (Da)
2.71
ALogP
7
HBA
1
HBD
105.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19N5O3
MW 365.39
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.51

Activity Summary

EC50 1 meas. best 7.62
IC50 1 meas. best 4.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Xanthine dehydrogenase/oxidase
CHEMBL3649
EC50 7.62 7.62 24.0 1
Xanthine dehydrogenase/oxidase
CHEMBL3649
IC50 4.62 4.62 24000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 985.52 nM Rattus norvegicus
T1/2 0.45 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19027292 10.1016/j.bmcl.2008.10.122 Rattus norvegicus 3
19027292 10.1016/j.bmcl.2008.10.122 Xanthine dehydrogenase/oxidase 1
19027292 10.1016/j.bmcl.2008.10.122 Cytochrome P450 3A4 1
29407989 10.1016/j.ejmech.2018.01.060 Xanthine dehydrogenase/oxidase 1

Data from ChEMBL 36 via Core Engine