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Compound Detail

CHEMBL219172

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

Basic Information

ChEMBL ID CHEMBL219172
Phase Preclinical
Structure Type MOL
InChI Key RDDFBAPIHCKOCC-UHFFFAOYSA-N
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

381.4
MW (Da)
4.08
ALogP
5
HBA
2
HBD
77.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24FN3O2
MW 381.45
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.93

Activity Summary

IC50 6 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
IC50 7.28 7.28 52.0 3
Acetylcholinesterase
CHEMBL220
IC50 6.72 6.7133 190.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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
19374444 10.1021/jm801292b Acetylcholinesterase 2
18640842 10.1016/j.bmc.2008.07.005 Acetylcholinesterase 2
17181144 10.1021/jm061047j Cholinesterase 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
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