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Compound Detail

CHEMBL374184

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CCOC(=O)C1=C(C)Nc2nc3c(c(N)c2C1c1ccc(OC)cc1)CCCC3

Basic Information

ChEMBL ID CHEMBL374184
Phase Preclinical
Structure Type MOL
InChI Key ZNRGREFWBCWZAU-UHFFFAOYSA-N
2
Targets
8
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
3.95
ALogP
6
HBA
2
HBD
86.5
PSA (Ų)
0.77
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N3O3
MW 393.49
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.64

Activity Summary

IC50 7 meas. best 7.35
Ki 1 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.35 7.0675 45.0 4
Acetylcholinesterase
CHEMBL4078
IC50 7.35 7.35 45.0 3
Acetylcholinesterase
CHEMBL220
Ki 6.96 6.96 109.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19374444 10.1021/jm801292b Acetylcholinesterase 5
17181144 10.1021/jm061047j SH-SY5Y 4
17181144 10.1021/jm061047j Acetylcholinesterase 2
17181144 10.1021/jm061047j Unchecked 2
19374444 10.1021/jm801292b SH-SY5Y 2
18640842 10.1016/j.bmc.2008.07.005 Acetylcholinesterase 2
17181144 10.1021/jm061047j Cholinesterase 1
18181565 10.1021/jm7009364 Acetylcholinesterase 1
19374444 10.1021/jm801292b Cholinesterases; ACHE & BCHE 1
19374444 10.1021/jm801292b ADMET 1
19374444 10.1021/jm801292b Voltage-gated L-type calcium channel 1
19374444 10.1021/jm801292b Cholinesterase 1
19374444 10.1021/jm801292b Unchecked 1
18640842 10.1016/j.bmc.2008.07.005 Cholinesterase 1
18640842 10.1016/j.bmc.2008.07.005 Unchecked 1

Data from ChEMBL 36 via Core Engine