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Compound Detail

CHEMBL2163794

OXYACANTHINE SULFATE
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COc1cc2c3cc1Oc1c(OO)c(OC)cc4c1[C@H](Cc1ccc(cc1)Oc1cc(ccc1O)C[C@H]3N(C)CC2)N(C)CC4.O=S(=O)(O)O

Basic Information

ChEMBL ID CHEMBL2163794
Name OXYACANTHINE SULFATE
Phase Preclinical
Structure Type MOL
InChI Key PVBVCFCKQXBCAB-CNORLSDQSA-N
Parent Compound CHEMBL2219880
Active Moiety CHEMBL2219880
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

610.7
MW (Da)
6.70
ALogP
9
HBA
2
HBD
93.1
PSA (Ų)
0.19
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H40N2O11S
MW 708.79
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness 2.02

Activity Summary

IC50 2 meas. best 5.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.72 5.72 1890.0 1
Cholinesterase
CHEMBL5763
IC50 5.39 5.39 4100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 1890.0 nM 5.72 Inhibition of human BChE by Ellman's method 23062825
Cholinesterase IC50 = 4100.0 nM 5.39 Inhibition of horse BChE by Ellman's method 23062825

Literature References

PubMed DOI Target Context # Activities
23062825 10.1016/j.bmc.2012.09.040 Cholinesterase 3
23062825 10.1016/j.bmc.2012.09.040 Acetylcholinesterase 2
23062825 10.1016/j.bmc.2012.09.040 Unchecked 1

Data from ChEMBL 36 via Core Engine