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Compound Detail

CHEMBL191314

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CNC(=O)Oc1cccc(CN(C)CCCCCCCOc2ccc3c(c2)O/C(=C\c2c4ccccc4cc4ccccc24)C3=O)c1

Basic Information

ChEMBL ID CHEMBL191314
Phase Preclinical
Structure Type MOL
InChI Key SGDJPNXFOBBUMA-HBAMXUDRSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

628.8
MW (Da)
8.79
ALogP
6
HBA
1
HBD
77.1
PSA (Ų)
0.08
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H40N2O5
MW 628.77
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -0.58

Activity Summary

IC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.1 5.6 79.1 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 79.1 nM 7.1 Inhibition of AChE 20053484
Acetylcholinesterase IC50 = 79100.0 nM 4.1 Inhibition of recombinant human AChE 15974596

Literature References

PubMed DOI Target Context # Activities
15974596 10.1021/jm049515h Acetylcholinesterase 2
15974596 10.1021/jm049515h Cholinesterase 1
15974596 10.1021/jm049515h Cholinesterases; ACHE & BCHE 1
15974596 10.1021/jm049515h No relevant target 1
20053484 10.1016/j.ejmech.2009.12.038 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine