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Compound Detail

CHEMBL174821

E129
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COc1cc(S(=O)(=O)[O-])c(C)cc1N=Nc1c(O)ccc2cc(S(=O)(=O)[O-])ccc12.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL174821
Name E129
Phase Preclinical
Structure Type MOL
InChI Key CEZCCHQBSQPRMU-UHFFFAOYSA-L
Parent Compound CHEMBL1206007
Active Moiety CHEMBL1206007
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
3.77
ALogP
8
HBA
3
HBD
162.9
PSA (Ų)
0.39
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H14N2Na2O8S2
MW 496.43
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.54

Activity Summary

IC50 3 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 4.48 4.48 33000.0 1
Unchecked
CHEMBL612545
IC50 4.05 4.05 90000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15050628 10.1016/j.bmcl.2004.01.079 Unchecked 1
15050628 10.1016/j.bmcl.2004.01.079 Tyrosine-protein phosphatase non-receptor type 1 1
15050628 10.1016/j.bmcl.2004.01.079 Tyrosine-protein phosphatase 1 1

Data from ChEMBL 36 via Core Engine