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Compound Detail

CHEMBL379437

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C=C(CC)C(=O)c1ccc(OCC(=O)NCCCCCCCCC(=O)NCc2cc(CNC(=O)CCCCCCCNC(=O)COc3ccc(C(O)C(=C)CC)c(Cl)c3Cl)cc(C(N)=O)c2)c(Cl)c1Cl

Basic Information

ChEMBL ID CHEMBL379437
Phase Preclinical
Structure Type MOL
InChI Key UQYZKFCWWOEUOK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

1048.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C52H67Cl4N5O9
MW 1047.95

Activity Summary

IC50 2 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutathione S-transferase P
CHEMBL3902
IC50 7.51 7.51 31.0 1
Glutathione S-transferase A1
CHEMBL3409
IC50 7.28 7.28 52.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutathione S-transferase P IC50 = 31.0 nM 7.51 Inhibition of GST P1-1 16675217
Glutathione S-transferase A1 IC50 = 52.1 nM 7.28 Inhibition of GST A1-1 16675217

Literature References

PubMed DOI Target Context # Activities
16675217 10.1016/j.bmcl.2006.04.041 Unchecked 1
16675217 10.1016/j.bmcl.2006.04.041 Glutathione S-transferase P 1
16675217 10.1016/j.bmcl.2006.04.041 Glutathione S-transferase A1 1

Data from ChEMBL 36 via Core Engine