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Compound Detail

CHEMBL117651

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Nc1ccc2c(c1)c(-c1ccccc1)[n+](CCCCCCc1cnnn1CCNc1c3c(nc4ccccc14)CCCC3)c1cc(N)ccc21

Basic Information

ChEMBL ID CHEMBL117651
Phase Preclinical
Structure Type MOL
InChI Key ISUOMOOYAOQQPZ-UHFFFAOYSA-O
3
Targets
7
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

661.9
MW (Da)
8.05
ALogP
7
HBA
3
HBD
111.5
PSA (Ų)
0.05
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C42H45N8+
MW 661.88
Aromatic Rings 7
Heavy Atoms 50
NP-Likeness -0.42

Activity Summary

Kd 4 meas.
Ki 3 meas. best 10.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4780
Ki 10.11 10.11 0.1 1
Acetylcholinesterase
CHEMBL3198
Ki 9.39 9.39 0.4 1
Cholinesterase
CHEMBL2528
Ki 9.14 9.14 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 0.077 nM 10.11 Inhibition of Torpedo californica AChE 18479118
Acetylcholinesterase Ki = 0.41 nM 9.39 Inhibition of mouse AChE 18479118
Cholinesterase Ki = 0.72 nM 9.14 Inhibition of mouse BuChE 18479118

Literature References

PubMed DOI Target Context # Activities
18479118 10.1021/jm701253t Acetylcholinesterase 2
29873484 10.1021/acs.jmedchem.8b00266 Acetylcholinesterase 2
15214773 10.1021/jm040031v Acetylcholinesterase 1
18479118 10.1021/jm701253t Cholinesterase 1
24811300 10.1016/j.bmc.2014.04.019 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine