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Compound Detail

CHEMBL3425892

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COc1cc(/C=C/c2ccc3ccccc3[n+]2C)ccc1N1CCOCC1.[I-]

Basic Information

ChEMBL ID CHEMBL3425892
Phase Preclinical
Structure Type MOL
InChI Key QNHHRZFBOWOGEJ-UHFFFAOYSA-M
Parent Compound CHEMBL3559268
Active Moiety CHEMBL3559268
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

361.5
MW (Da)
3.68
ALogP
3
HBA
0
HBD
25.6
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25IN2O2
MW 488.37
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.57

Activity Summary

IC50 3 meas. best 5.72
Kd 1 meas. best 4.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.72 5.72 1900.0 1
Unchecked
CHEMBL612545
Kd 4.55 4.55 28200.0 1
HeLa
CHEMBL399
IC50 4.48 4.48 32800.0 1
ADMET
CHEMBL612558
IC50 4.31 4.31 49100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25822852 10.1021/acs.jmedchem.5b00139 Unchecked 3
28242549 10.1016/j.ejmech.2017.02.042 No relevant target 2
28242549 10.1016/j.ejmech.2017.02.042 Acetylcholinesterase 2
28242549 10.1016/j.ejmech.2017.02.042 Cholinesterase 2
25822852 10.1021/acs.jmedchem.5b00139 HeLa 1
25822852 10.1021/acs.jmedchem.5b00139 ADMET 1
28242549 10.1016/j.ejmech.2017.02.042 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine