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Compound Detail

CHEMBL208604

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O=C1C[C@@H](c2ccc(C[C@H](NS(=O)(=O)c3ccccc3)c3nc4ccccc4[nH]3)cc2Cl)S(=O)(=O)[N-]1.[Na+]

Basic Information

ChEMBL ID CHEMBL208604
Phase Preclinical
Structure Type MOL
InChI Key KFHSGHCVUQSXFH-VROPFNGYSA-M
Parent Compound CHEMBL1206098
Active Moiety CHEMBL1206098
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

545.0
MW (Da)
3.37
ALogP
6
HBA
3
HBD
138.1
PSA (Ų)
0.33
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 C24H20ClN4NaO5S2
MW 567.02
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.18

Activity Summary

IC50 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 7.3 7.3 50.0 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 = 50.0 nM 7.3 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 2
16789735 10.1021/jm0600904 Caco-2 1

Data from ChEMBL 36 via Core Engine