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Compound Detail

CHEMBL3632853

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COc1ccc(-c2cc3c(c(=O)o2)C[C@]2(O)[C@@]4(C)CC[C@@H](OC(C)=O)C(C)(C)[C@]4(O)CC[C@@]2(C)O3)cc1

Basic Information

ChEMBL ID CHEMBL3632853
Phase Preclinical
Structure Type MOL
InChI Key LHKWCVMCNOROFZ-MCPFUKIPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
4.02
ALogP
8
HBA
2
HBD
115.4
PSA (Ų)
0.59
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C29H36O8
MW 512.60
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 1.86

Activity Summary

IC50 1 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 3500.0 nM 5.46 Inhibition of human AChE 26159481

Literature References

PubMed DOI Target Context # Activities
31433188 10.1021/acs.jnatprod.9b00563 Acetylcholinesterase 2
26159481 10.1016/j.bmcl.2015.06.047 Acetylcholinesterase 1
31433188 10.1021/acs.jnatprod.9b00563 Danio rerio 1
31433188 10.1021/acs.jnatprod.9b00563 Cholinesterase 1

Data from ChEMBL 36 via Core Engine