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Compound Detail

CHEMBL1096939

KUWANON E
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CC(C)=CCC/C(C)=C/Cc1cc(C2CC(=O)c3c(O)cc(O)cc3O2)c(O)cc1O

Basic Information

ChEMBL ID CHEMBL1096939
Name KUWANON E
Phase Preclinical
Structure Type MOL
InChI Key GJFHZVPRFLHEBR-VIZOYTHASA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

424.5
MW (Da)
5.45
ALogP
6
HBA
4
HBD
107.2
PSA (Ų)
0.46
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C25H28O6
MW 424.49
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 2.46

Activity Summary

IC50 2 meas. best 5.77
Ki 1 meas. best 5.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.77 5.77 1700.0 1
Acetylcholinesterase
CHEMBL220
Ki 5.51 5.51 3100.0 1
THP-1
CHEMBL614245
IC50 5.4 5.4 4000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 1700.0 nM 5.77 Inhibition of BuChE (unknown origin) -
Acetylcholinesterase Ki = 3100.0 nM 5.51 Inhibition of AChE (unknown origin) -
THP-1 IC50 = 4000.0 nM 5.4 Cytotoxicity against human THP1 cells after 24 hrs by WST1 assay 24901948

Literature References

PubMed DOI Target Context # Activities
24901948 10.1021/np401025f NON-PROTEIN TARGET 2
20192247 10.1021/np900681y MCF7 1
20192247 10.1021/np900681y CCRF-CEM 1
20192247 10.1021/np900681y RPMI-8226 1
20192247 10.1021/np900681y U-266 1
20192247 10.1021/np900681y HeLa 1
20192247 10.1021/np900681y BJ 1
20192247 10.1021/np900681y THP-1 1
- 10.1007/s00044-012-0353-y Cholinesterase 1
- 10.1007/s00044-012-0353-y Acetylcholinesterase 1
24901948 10.1021/np401025f THP-1 1

Data from ChEMBL 36 via Core Engine