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Compound Detail

CHEMBL5401594

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COc1cc2c3c(c1OC)-c1ccccc1C[C@H]3N(C(=O)c1cc[n+](Cc3ccccc3)cc1)CC2.[Br-]

Basic Information

ChEMBL ID CHEMBL5401594
Phase Preclinical
Structure Type MOL
InChI Key NUOZFMODYLYTKG-UFTMZEDQSA-M
Parent Compound CHEMBL5498550
Active Moiety CHEMBL5498550
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

477.6
MW (Da)
5.00
ALogP
3
HBA
0
HBD
42.6
PSA (Ų)
0.38
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H29BrN2O3
MW 557.49
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness 0.18

Activity Summary

IC50 2 meas. best 5.3
Ki 1 meas. best 5.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
Ki 5.59 5.59 2570.0 1
Cholinesterase
CHEMBL5763
IC50 5.3 5.3 4950.0 1
Acetylcholinesterase
CHEMBL4078
IC50 5.15 5.15 7150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38229749 10.1021/acsmedchemlett.3c00467 Acetylcholinesterase 2
38229749 10.1021/acsmedchemlett.3c00467 Cholinesterase 1
38229749 10.1021/acsmedchemlett.3c00467 Unchecked 1
38229749 10.1021/acsmedchemlett.3c00467 MRC5 1
38229749 10.1021/acsmedchemlett.3c00467 No relevant target 1

Data from ChEMBL 36 via Core Engine