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Compound Detail

CHEMBL234499

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N=C(Nc1ccc2nc(NC3CCN(Cc4ccc(C(=O)O)cc4)CC3)sc2c1)c1cccs1

Basic Information

ChEMBL ID CHEMBL234499
Phase Preclinical
Structure Type MOL
InChI Key RDEJBAAVSOBTGG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
5.57
ALogP
7
HBA
4
HBD
101.3
PSA (Ų)
0.20
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 C25H25N5O2S2
MW 491.64
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.91

Activity Summary

IC50 2 meas. best 5.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nitric oxide synthase 1
CHEMBL3568
IC50 5.29 5.29 5100.0 1
Nitric oxide synthase 3
CHEMBL4803
IC50 4.23 4.23 59000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nitric oxide synthase 1 IC50 = 5100.0 nM 5.29 Inhibition of human neuronal NOS activity 17317165
Nitric oxide synthase 3 IC50 = 59000.0 nM 4.23 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