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Compound Detail

CHEMBL191461

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CNC(=O)Oc1cccc(CN(C)CCCCCCCOc2ccc3c(c2)C/C(=C\c2cc(OC)c(OC)c(OC)c2)C3=O)c1

Basic Information

ChEMBL ID CHEMBL191461
Phase Preclinical
Structure Type MOL
InChI Key KYVIWBPYFDCUME-MTDXEUNCSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

616.8
MW (Da)
6.71
ALogP
8
HBA
1
HBD
95.6
PSA (Ų)
0.14
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H44N2O7
MW 616.75
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.46

Activity Summary

IC50 3 meas. best 5.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.75 5.75 1800.0 1
Cholinesterase
CHEMBL1914
IC50 4.09 4.09 81300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 1800.0 nM 5.75 Inhibition of recombinant human AChE 15974596
Cholinesterase IC50 = 81300.0 nM 4.09 Inhibition of isolated human BuChE 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
- 10.1007/s00044-010-9373-7 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine