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Compound Detail

CHEMBL4101303

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COc1cc2c(cc1OC)C(=O)C(CC1C=CN(Cc3cccc(Cl)c3)C=C1C(N)=O)C2

Basic Information

ChEMBL ID CHEMBL4101303
Phase Preclinical
Structure Type MOL
InChI Key JEGKSGQGZBQTIZ-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
2
PK Parameters
9
Publications
0
Known Names

Molecular Properties

452.9
MW (Da)
4.12
ALogP
5
HBA
1
HBD
81.9
PSA (Ų)
0.68
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25ClN2O4
MW 452.94
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.09

Activity Summary

IC50 4 meas. best 5.27
EC50 1 meas. best 4.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.27 4.92 5339.0 2
Cholinesterase
CHEMBL5763
IC50 4.84 4.77 14295.0 2
No relevant target
CHEMBL2362975
EC50 4.05 4.05 90000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.41 hr -
T1/2 0.295 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28613859 10.1021/acs.jmedchem.7b00702 Mus musculus 12
28613859 10.1021/acs.jmedchem.7b00702 No relevant target 8
28613859 10.1021/acs.jmedchem.7b00702 Brain 3
29324339 10.1016/j.ejmech.2017.12.084 Acetylcholinesterase 3
29324339 10.1016/j.ejmech.2017.12.084 Cholinesterase 3
28613859 10.1021/acs.jmedchem.7b00702 Salmonella typhimurium 2
29324339 10.1016/j.ejmech.2017.12.084 No relevant target 2
28613859 10.1021/acs.jmedchem.7b00702 Acetylcholinesterase 1
28613859 10.1021/acs.jmedchem.7b00702 Plasma 1

Data from ChEMBL 36 via Core Engine