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Compound Detail

CHEMBL221992

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CC[N+](C)(CCCCCC(=O)N1CCC(CCCC2CCN(C(=O)CCCCC[N+](C)(CC)Cc3ccccc3OC)CC2)CC1)Cc1ccccc1OC.[I-].[I-]

Basic Information

ChEMBL ID CHEMBL221992
Phase Preclinical
Structure Type MOL
InChI Key XMNUJBWKWUZYAE-UHFFFAOYSA-L
Parent Compound CHEMBL1182211
Active Moiety CHEMBL1182211
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

763.2
MW (Da)
9.11
ALogP
4
HBA
0
HBD
59.1
PSA (Ų)
0.08
QED
2
Ro5 Violations
24
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C47H78I2N4O4
MW 1016.97
Aromatic Rings 2
Heavy Atoms 55
NP-Likeness -0.09

Activity Summary

IC50 2 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 8.24 8.24 5.8 1
Cholinesterase
CHEMBL1914
IC50 6.18 6.18 660.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 5.754 nM 8.24 Inhibition of human recombinant AChE 15588084
Cholinesterase IC50 = 660.69 nM 6.18 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