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Compound Detail

CHEMBL19949

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CC[N+](C)(CCCCCC(=O)N1CCC(CCC2CCN(C(=O)CCCCC[N+](C)(CC)Cc3ccccc3OC)CC2)CC1)Cc1ccccc1OC.[I-].[I-]

Basic Information

ChEMBL ID CHEMBL19949
Phase Preclinical
Structure Type MOL
InChI Key CIYMTGNBOMNRQZ-UHFFFAOYSA-L
Parent Compound CHEMBL1178316
Active Moiety CHEMBL1178316
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

749.1
MW (Da)
8.72
ALogP
4
HBA
0
HBD
59.1
PSA (Ų)
0.08
QED
2
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H76I2N4O4
MW 1002.95
Aromatic Rings 2
Heavy Atoms 54
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 5.73 5.73 1862.1 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 = 1862.09 nM 5.73 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