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Compound Detail

CHEMBL599111

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COc1ccc(CCNc2nnc(Sc3ncc([N+](=O)[O-])s3)s2)cc1OC

Basic Information

ChEMBL ID CHEMBL599111
Phase Preclinical
Structure Type MOL
InChI Key IFYDDUABVTWOCJ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

425.5
MW (Da)
3.73
ALogP
11
HBA
1
HBD
112.3
PSA (Ų)
0.40
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N5O4S3
MW 425.52
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.59

Activity Summary

IC50 2 meas. best 7.0
Kd 1 meas. best 5.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 7.0 7.0 100.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
Kd 5.72 5.72 1900.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.24 5.24 5700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20045647 10.1016/j.bmc.2009.12.013 Plasma 2
20045647 10.1016/j.bmc.2009.12.013 Mitogen-activated protein kinase 9 2
20045647 10.1016/j.bmc.2009.12.013 Mitogen-activated protein kinase 8 1
20045647 10.1016/j.bmc.2009.12.013 ADMET 1
20045647 10.1016/j.bmc.2009.12.013 Mitogen-activated protein kinase 14 1
20045647 10.1016/j.bmc.2009.12.013 RAC-alpha serine/threonine-protein kinase 1
20045647 10.1016/j.bmc.2009.12.013 Furin 1
20045647 10.1016/j.bmc.2009.12.013 Lethal factor 1

Data from ChEMBL 36 via Core Engine