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Compound Detail

CHEMBL222043

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CC[N+](C)(CCCCCC(=O)Nc1ccc(CCc2ccc(NC(=O)CCCCC[N+](C)(CC)Cc3ccccc3OC)cc2)cc1)Cc1ccccc1OC.[I-].[I-]

Basic Information

ChEMBL ID CHEMBL222043
Phase Preclinical
Structure Type MOL
InChI Key WYCCMMPZBMSCAC-UHFFFAOYSA-N
Parent Compound CHEMBL1182212
Active Moiety CHEMBL1182212
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

765.1
MW (Da)
9.82
ALogP
4
HBA
2
HBD
76.7
PSA (Ų)
0.05
QED
2
Ro5 Violations
25
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H68I2N4O4
MW 1018.90
Aromatic Rings 4
Heavy Atoms 56
NP-Likeness -0.18

Activity Summary

IC50 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.92 6.92 120.2 1
Cholinesterase
CHEMBL1914
IC50 5.96 5.96 1096.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 120.23 nM 6.92 Inhibition of human recombinant AChE 15588084
Cholinesterase IC50 = 1096.48 nM 5.96 Inhibition of human recombinant BChE 15588084

Literature References

PubMed DOI Target Context # Activities
15588084 10.1021/jm0494366 Acetylcholinesterase 2
15588084 10.1021/jm0494366 Cholinesterase 1
15588084 10.1021/jm0494366 Cholinesterases; ACHE & BCHE 1
15588084 10.1021/jm0494366 Muscarinic acetylcholine receptor M2 1

Data from ChEMBL 36 via Core Engine