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Compound Detail

CHEMBL222340

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CCN(CCCCCC(=O)Nc1ccc(-c2ccc(NC(=O)CCCCCN(CC)Cc3ccccc3OC)cc2)cc1)Cc1ccccc1OC.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL222340
Phase Preclinical
Structure Type MOL
InChI Key IQFIVNLEJJKLBW-UHFFFAOYSA-N
Parent Compound CHEMBL403260
Active Moiety CHEMBL403260
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

707.0
MW (Da)
9.41
ALogP
6
HBA
2
HBD
83.1
PSA (Ų)
0.07
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 C46H60N4O8
MW 797.01
Aromatic Rings 4
Heavy Atoms 52
NP-Likeness -0.65

Activity Summary

IC50 2 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.44 7.44 36.3 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 = 36.31 nM 7.44 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