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Compound Detail

CHEMBL3917990

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COc1ccc(/C=C/C(=O)Nc2ccc(CN(C)Cc3ccccc3)cc2)cc1OC

Basic Information

ChEMBL ID CHEMBL3917990
Phase Preclinical
Structure Type MOL
InChI Key SBRJGGDKKJIEFJ-FOWTUZBSSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
4.99
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.50
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28N2O3
MW 416.52
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.80

Activity Summary

IC50 5 meas. best 5.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.81 5.81 1560.0 1
Acetylcholinesterase
CHEMBL4078
IC50 5.71 5.71 1940.0 1
Acetylcholinesterase
CHEMBL220
IC50 5.53 5.465 2960.0 2
Cholinesterase
CHEMBL5763
IC50 5.43 5.43 3720.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28800459 10.1016/j.ejmech.2017.07.077 Acetylcholinesterase 2
28800459 10.1016/j.ejmech.2017.07.077 Cholinesterase 2
28800459 10.1016/j.ejmech.2017.07.077 No relevant target 2
27267007 10.1016/j.ejmech.2016.05.055 Cholinesterase 1
27267007 10.1016/j.ejmech.2016.05.055 Acetylcholinesterase 1
27267007 10.1016/j.ejmech.2016.05.055 Amine oxidase [flavin-containing] A 1
27267007 10.1016/j.ejmech.2016.05.055 Amine oxidase [flavin-containing] B 1
27267007 10.1016/j.ejmech.2016.05.055 No relevant target 1
28800459 10.1016/j.ejmech.2017.07.077 Unchecked 1
28800459 10.1016/j.ejmech.2017.07.077 Cholinesterases; ACHE & BCHE 1
28800459 10.1016/j.ejmech.2017.07.077 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine