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Compound Detail

CHEMBL1081032

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CN1c2ccc(OC(=O)NCC3CCCCC3)cc2[C@]2(C)CCN(CCc3ccccc3)[C@H]12

Basic Information

ChEMBL ID CHEMBL1081032
Phase Preclinical
Structure Type MOL
InChI Key OSMWANBXVVPETF-XCZPVHLTSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
5.34
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.65
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H37N3O2
MW 447.62
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.14

Activity Summary

IC50 6 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 8.74 8.74 1.8 2
Acetylcholinesterase
CHEMBL220
IC50 8.74 7.17 1.8 2
Cholinesterase
CHEMBL2528
IC50 8.74 8.74 1.8 1
Acetylcholinesterase
CHEMBL3198
IC50 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20137941 10.1016/j.bmcl.2010.01.035 Acetylcholinesterase 1
20137941 10.1016/j.bmcl.2010.01.035 Cholinesterase 1
20137941 10.1016/j.bmcl.2010.01.035 Unchecked 1
34923430 10.1016/j.ejmech.2021.114044 Acetylcholinesterase 1
34923430 10.1016/j.ejmech.2021.114044 Cholinesterase 1
35858523 10.1016/j.ejmech.2022.114606 Acetylcholinesterase 1
35858523 10.1016/j.ejmech.2022.114606 Cholinesterase 1
35858523 10.1016/j.ejmech.2022.114606 Cholinesterases; ACHE & BCHE 1

Data from ChEMBL 36 via Core Engine