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Compound Detail

CHEMBL3754370

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Cc1nc(-c2cc3cc(OC(C)C)cc([N+](=O)[O-])c3[nH]2)sc1C(=O)O

Basic Information

ChEMBL ID CHEMBL3754370
Phase Preclinical
Structure Type MOL
InChI Key CJZRKAZYEVMXSR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
3.99
ALogP
6
HBA
2
HBD
118.3
PSA (Ų)
0.52
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 C16H15N3O5S
MW 361.38
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.60

Activity Summary

IC50 1 meas. best 8.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.29 8.29 5.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 8230.0 ng.hr.mL-1 Rattus norvegicus
AUC 13140.0 ng.hr.mL-1 Rattus norvegicus
Cmax 13669.82 nM Rattus norvegicus
T1/2 4.127 hr Rattus norvegicus
T1/2 3.45 hr Rattus norvegicus
Tmax 0.42 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 5.1 nM 8.29 Inhibition of butter milk xanthine oxidase (unknown origin) assessed as initial ... 26774578

Literature References

PubMed DOI Target Context # Activities
26774578 10.1016/j.bmcl.2015.12.055 Rattus norvegicus 6
26774578 10.1016/j.bmcl.2015.12.055 Unchecked 1
26774578 10.1016/j.bmcl.2015.12.055 Liver microsome 1

Data from ChEMBL 36 via Core Engine