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Compound Detail

CHEMBL233024

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N=C(Nc1ccc2sc(NCCN3CCOCC3)nc2c1)c1cccs1

Basic Information

ChEMBL ID CHEMBL233024
Phase Preclinical
Structure Type MOL
InChI Key SCCBBFJXHRRFRM-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
3.54
ALogP
7
HBA
3
HBD
73.3
PSA (Ų)
0.45
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21N5OS2
MW 387.53
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -2.64

Activity Summary

IC50 3 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nitric oxide synthase 1
CHEMBL3568
IC50 5.89 5.89 1300.0 1
Nitric oxide synthase 3
CHEMBL4803
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nitric oxide synthase 1 IC50 = 1300.0 nM 5.89 Inhibition of human neuronal NOS activity 17317165
Nitric oxide synthase 3 IC50 = 12000.0 nM 4.92 Inhibition of human endothelial NOS activity 17317165

Literature References

PubMed DOI Target Context # Activities
17317165 10.1016/j.bmcl.2007.02.011 Nitric oxide synthase 1 1
17317165 10.1016/j.bmcl.2007.02.011 Nitric oxide synthase 3 1
17317165 10.1016/j.bmcl.2007.02.011 Nitric oxide synthase, inducible 1
17317165 10.1016/j.bmcl.2007.02.011 Unchecked 1
17317165 10.1016/j.bmcl.2007.02.011 Nitric oxide sythases; iNOS & nNOS 1

Data from ChEMBL 36 via Core Engine