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Compound Detail

CHEMBL4541077

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COc1ccc2[nH]cc(CCNC(=O)CN(CCCC3CCN(Cc4ccccc4)CC3)C(=O)/C=C/c3ccc(O)c(OC)c3)c2c1

Basic Information

ChEMBL ID CHEMBL4541077
Phase Preclinical
Structure Type MOL
InChI Key XCEUHRXQIRAKKN-RVDMUPIBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

638.8
MW (Da)
5.78
ALogP
6
HBA
3
HBD
107.1
PSA (Ų)
0.14
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H46N4O5
MW 638.81
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.60

Activity Summary

IC50 2 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 7.76 7.76 17.5 1
Acetylcholinesterase
CHEMBL220
IC50 7.58 7.58 26.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 17.5 nM 7.76 Inhibition of human butyrylcholinesterase 30744931
Acetylcholinesterase IC50 = 26.2 nM 7.58 Inhibition of human acetylcholinesterase 30744931

Literature References

PubMed DOI Target Context # Activities
30744931 10.1016/j.bmc.2019.01.025 Acetylcholinesterase 1
30744931 10.1016/j.bmc.2019.01.025 Cholinesterase 1

Data from ChEMBL 36 via Core Engine