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Compound Detail

CHEMBL403650

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CC(C)(C)CCn1c(=O)c(C2=NS(=O)(=O)c3cc(NS(C)(=O)=O)ccc3N2)c(O)c2cccn21

Basic Information

ChEMBL ID CHEMBL403650
Phase Preclinical
Structure Type MOL
InChI Key FCKKBGLFVWWSIL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
6
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
2.18
ALogP
9
HBA
3
HBD
151.3
PSA (Ų)
0.48
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N5O6S2
MW 507.59
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.13

Activity Summary

EC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatitis C virus
CHEMBL379
EC50 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 25.0 ng.hr.mL-1 Macaca fascicularis
AUC 1209.0 ng.hr.mL-1 Macaca fascicularis
CL 14.0 mL.min-1.kg-1 Macaca fascicularis
F 2.0 % Macaca fascicularis
T1/2 0.1667 hr Homo sapiens
T1/2 0.2333 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatitis C virus EC50 = 5.0 nM 8.3 Antiviral activity against HCV 1b in human Huh7/C24 cells after 72 hrs by replic... 18487044

Literature References

PubMed DOI Target Context # Activities
18487044 10.1016/j.bmcl.2008.04.066 Cynomolgus monkey 4
18487044 10.1016/j.bmcl.2008.04.066 Hepatitis C virus 2
18487044 10.1016/j.bmcl.2008.04.066 ADMET 2
18487044 10.1016/j.bmcl.2008.04.066 Liver microsomes 1
18487044 10.1016/j.bmcl.2008.04.066 No relevant target 1
18487044 10.1016/j.bmcl.2008.04.066 Caco-2 1

Data from ChEMBL 36 via Core Engine