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Compound Detail

CHEMBL1814730

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Cl.O=C(NCCCNc1c2c(nc3ccccc13)CCCC2)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL1814730
Phase Preclinical
Structure Type MOL
InChI Key PAINQULSLLEVJB-UHFFFAOYSA-N
Parent Compound CHEMBL1851881
Active Moiety CHEMBL1851881
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

377.5
MW (Da)
4.48
ALogP
3
HBA
2
HBD
54.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClFN3O
MW 413.92
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.27

Activity Summary

IC50 2 meas. best 10.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 10.67 10.67 0.0 1
Acetylcholinesterase
CHEMBL220
IC50 9.09 9.09 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 0.0212 nM 10.67 Inhibition of BChE by Ellman's method 21570751
Acetylcholinesterase IC50 = 0.809 nM 9.09 Inhibition of AChE by Ellman's method 21570751

Literature References

PubMed DOI Target Context # Activities
21570751 10.1016/j.ejmech.2011.04.038 Acetylcholinesterase 2
21570751 10.1016/j.ejmech.2011.04.038 Unchecked 2
21570751 10.1016/j.ejmech.2011.04.038 Cholinesterase 1

Data from ChEMBL 36 via Core Engine