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Compound Detail

CHEMBL5597984

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O=C(O)[C@@H]1[C@@H](OCCc2ccccc2)[C@H](O)[C@@H](O)c2nc(CCc3cccc(Oc4ccccc4)c3)cn21

Basic Information

ChEMBL ID CHEMBL5597984
Phase Preclinical
Structure Type MOL
InChI Key WKAPFHFZEZLTLU-KUXCXQDQSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

514.6
MW (Da)
4.12
ALogP
7
HBA
3
HBD
114.0
PSA (Ų)
0.29
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30N2O6
MW 514.58
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness 0.16

Activity Summary

IC50 3 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heparanase
CHEMBL3921
IC50 7.24 7.24 57.0 1
Unchecked
CHEMBL612545
IC50 5.9 5.9 1250.0 1
Beta-glucuronidase
CHEMBL2728
IC50 5.14 5.14 7210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Heparanase IC50 = 57.0 nM 7.24 Inhibition of HPSE1 (unknown origin) 37939863
Unchecked IC50 = 1250.0 nM 5.9 Inhibition of GBA (unknown origin) 37939863
Beta-glucuronidase IC50 = 7210.0 nM 5.14 Inhibition of GUSbeta (unknown origin) 37939863

Literature References

PubMed DOI Target Context # Activities
37939863 10.1016/j.bmcl.2023.129543 Heparanase 1
37939863 10.1016/j.bmcl.2023.129543 Beta-glucuronidase 1
37939863 10.1016/j.bmcl.2023.129543 Unchecked 1

Data from ChEMBL 36 via Core Engine