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Compound Detail

CHEMBL374772

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CN(C)C(N)(N)OS(=O)(=O)O/C=C1/CC[C@H]2[C@](C)(CC[C@H]3C(C)(C)CCC[C@]23C)[C@H]1CCc1ccoc1

Basic Information

ChEMBL ID CHEMBL374772
Phase Preclinical
Structure Type MOL
InChI Key GNRJWJGZOYSPRS-DEJOVQTRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

537.8
MW (Da)
5.12
ALogP
8
HBA
2
HBD
121.0
PSA (Ų)
0.35
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H47N3O5S
MW 537.77
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 2.02

Activity Summary

IC50 2 meas. best 5.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.25 5.25 5600.0 1
UDP-glucose 4-epimerase
CHEMBL5843
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 5600.0 nM 5.25 Inhibition of Trypanosoma brucei GalE by HPAEC assay 16962325
UDP-glucose 4-epimerase IC50 = 12000.0 nM 4.92 Inhibition of human GalE by HPAEC assay 16962325

Literature References

PubMed DOI Target Context # Activities
16962325 10.1016/j.bmcl.2006.08.091 Unchecked 2
16962325 10.1016/j.bmcl.2006.08.091 UDP-glucose 4-epimerase 1
16962325 10.1016/j.bmcl.2006.08.091 Trypanosoma brucei 1
16962325 10.1016/j.bmcl.2006.08.091 CHO-K1 1

Data from ChEMBL 36 via Core Engine