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Compound Detail

CHEMBL377989

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Cc1cc(C[C@H](NS(=O)(=O)c2ccccc2)c2nc3ccccc3[nH]2)ccc1[C@@H]1CC(=O)[N-]S1(=O)=O.[Na+]

Basic Information

ChEMBL ID CHEMBL377989
Phase Preclinical
Structure Type MOL
InChI Key RBMPKEPGBTZDSR-SJEIDVEUSA-M
Parent Compound CHEMBL248291
Active Moiety CHEMBL248291
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

524.6
MW (Da)
3.02
ALogP
6
HBA
3
HBD
138.1
PSA (Ų)
0.34
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 C25H23N4NaO5S2
MW 546.61
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 7.46 7.46 35.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein phosphatase non-receptor type 1 IC50 = 35.0 nM 7.46 Inhibition of PTP1B by pNPP assay 16789735

Literature References

PubMed DOI Target Context # Activities
16789735 10.1021/jm0600904 Tyrosine-protein phosphatase non-receptor type 1 9
16789735 10.1021/jm0600904 Caco-2 1

Data from ChEMBL 36 via Core Engine