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Compound Detail

CHEMBL212685

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

Basic Information

ChEMBL ID CHEMBL212685
Phase Preclinical
Structure Type MOL
InChI Key FGDHVUMZJFNQIL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

863.6
MW (Da)
5.32
ALogP
9
HBA
5
HBD
212.1
PSA (Ų)
0.07
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H39Cl4N5O9
MW 863.58
Aromatic Rings 3
Heavy Atoms 57
NP-Likeness -0.46

Activity Summary

IC50 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutathione S-transferase A1
CHEMBL3409
IC50 7.62 7.62 24.0 1
Glutathione S-transferase P
CHEMBL3902
IC50 6.15 6.15 704.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutathione S-transferase A1 IC50 = 24.0 nM 7.62 Inhibition of GST A1-1 16675217
Glutathione S-transferase P IC50 = 704.0 nM 6.15 Inhibition of GST P1-1 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