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Compound Detail

CHEMBL503022

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O=[N+]([O-])c1cnc(Sc2nnc(Sc3ncc([N+](=O)[O-])s3)s2)s1

Basic Information

ChEMBL ID CHEMBL503022
Phase Preclinical
Structure Type MOL
InChI Key QYKQHNTWQJPQOZ-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

406.5
MW (Da)
3.57
ALogP
13
HBA
0
HBD
137.8
PSA (Ų)
0.44
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C8H2N6O4S5
MW 406.48
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.28

Activity Summary

IC50 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.1 7.915 0.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.8 nM 9.1 Inhibition of JNK by time-resolved FRET assay 19271755
Unchecked IC50 = 187.0 nM 6.73 Displacement of biotin-labeled pep-JIP11 from JNK by DELFIA assay 19271755

Literature References

PubMed DOI Target Context # Activities
19271755 10.1021/jm801503n Unchecked 3
19271755 10.1021/jm801503n Mitogen-activated protein kinase 14 1
19271755 10.1021/jm801503n RAC-alpha serine/threonine-protein kinase 1
19271755 10.1021/jm801503n Furin 1

Data from ChEMBL 36 via Core Engine