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Compound Detail

CHEMBL4756491

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COc1ccc2cc3[n+](cc2c1OCc1ccccc1C)CCc1cc2c(cc1-3)OCO2.[Br-]

Basic Information

ChEMBL ID CHEMBL4756491
Phase Preclinical
Structure Type MOL
InChI Key SASXDYIDYKHAHB-UHFFFAOYSA-M
Parent Compound CHEMBL4802927
Active Moiety CHEMBL4802927
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

426.5
MW (Da)
4.98
ALogP
4
HBA
0
HBD
40.8
PSA (Ų)
0.43
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24BrNO4
MW 506.40
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness 0.69

Activity Summary

IC50 4 meas. best 4.98
EC50 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 4.98 4.98 10400.0 1
Cholinesterase
CHEMBL1914
IC50 4.67 4.67 21500.0 1
CHO-K1
CHEMBL614031
IC50 4.26 4.26 55000.0 1
Prolyl endopeptidase
CHEMBL3202
IC50 4.15 4.15 71100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32688201 10.1016/j.ejmech.2020.112593 Prolyl endopeptidase 1
32688201 10.1016/j.ejmech.2020.112593 Unchecked 1
32688201 10.1016/j.ejmech.2020.112593 Acetylcholinesterase 1
32688201 10.1016/j.ejmech.2020.112593 Cholinesterase 1
32688201 10.1016/j.ejmech.2020.112593 CHO-K1 1
32688201 10.1016/j.ejmech.2020.112593 No relevant target 1

Data from ChEMBL 36 via Core Engine