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Compound Detail

CHEMBL514534

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Cc1c(C)c2ccc(OCCCOc3cc(O)cc([N+](C)(C)C)c3)cc2oc1=O.[I-]

Basic Information

ChEMBL ID CHEMBL514534
Phase Preclinical
Structure Type MOL
InChI Key ANOBKSRPWWJDLQ-UHFFFAOYSA-N
Parent Compound CHEMBL1187667
Active Moiety CHEMBL1187667
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

398.5
MW (Da)
4.16
ALogP
5
HBA
1
HBD
68.9
PSA (Ų)
0.37
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28INO5
MW 525.38
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 0.24

Activity Summary

IC50 2 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4768
IC50 8.68 8.68 2.1 1
Cholinesterase
CHEMBL5763
IC50 5.97 5.97 1060.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 2.1 nM 8.68 Inhibition of bovine AChE by Ellman's method 18585045
Cholinesterase IC50 = 1060.0 nM 5.97 Inhibition of equine BChE by Ellman's method 18585045

Literature References

PubMed DOI Target Context # Activities
18585045 10.1016/j.bmc.2008.06.022 Acetylcholinesterase 1
18585045 10.1016/j.bmc.2008.06.022 Cholinesterase 1
18585045 10.1016/j.bmc.2008.06.022 Unchecked 1

Data from ChEMBL 36 via Core Engine