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Compound Detail

CHEMBL199454

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COc1ccc2[nH]cc(CCNC(=O)CCCCCNc3c4c(nc5ccccc35)CCCC4)c2c1

Basic Information

ChEMBL ID CHEMBL199454
Phase Preclinical
Structure Type MOL
InChI Key BGQKPFJETYONAB-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
5.93
ALogP
4
HBA
3
HBD
79.0
PSA (Ų)
0.23
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N4O2
MW 484.64
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.67

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Butyrylcholinesterase
CHEMBL5077
IC50 8.7 8.7 2.0 1
Acetylcholinesterase
CHEMBL4768
IC50 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Butyrylcholinesterase IC50 = 2.0 nM 8.7 Inhibition of BuChE from horse serum 16420031
Acetylcholinesterase IC50 = 9.0 nM 8.05 Inhibition of AchE from bovine erythrocytes 16420031

Literature References

PubMed DOI Target Context # Activities
30744931 10.1016/j.bmc.2019.01.025 Acetylcholinesterase 2
16420031 10.1021/jm050746d Acetylcholinesterase 1
16420031 10.1021/jm050746d Butyrylcholinesterase 1
16420031 10.1021/jm050746d ADMET 1

Data from ChEMBL 36 via Core Engine