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Compound Detail

CHEMBL257750

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CS(=O)(=O)Nc1ccc2c(c1)S(=O)(=O)N=C(c1c(O)c(C3=CCCC3)nn(CCC3CC3)c1=O)N2

Basic Information

ChEMBL ID CHEMBL257750
Phase Preclinical
Structure Type MOL
InChI Key CLCXAYCXXFZWQG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

519.6
MW (Da)
2.25
ALogP
9
HBA
3
HBD
159.8
PSA (Ų)
0.50
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N5O6S2
MW 519.61
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.00

Activity Summary

EC50 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatitis C virus
CHEMBL379
EC50 7.66 7.66 22.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 4.0 % Macaca fascicularis
T1/2 0.5167 hr Homo sapiens
T1/2 0.6833 hr Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatitis C virus EC50 = 22.0 nM 7.66 Antiviral activity against HCV 1b replicon in human Huh7/C24 cells after 72 hrs 18442904

Literature References

PubMed DOI Target Context # Activities
18442904 10.1016/j.bmcl.2008.04.005 ADMET 2
18442904 10.1016/j.bmcl.2008.04.005 Caco-2 2
18442904 10.1016/j.bmcl.2008.04.005 Cynomolgus monkey 2
18442904 10.1016/j.bmcl.2008.04.005 Hepatitis C virus 1
18442904 10.1016/j.bmcl.2008.04.005 Liver microsomes 1
18442904 10.1016/j.bmcl.2008.04.005 No relevant target 1

Data from ChEMBL 36 via Core Engine