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Compound Detail

CHEMBL365136

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

Basic Information

ChEMBL ID CHEMBL365136
Phase Preclinical
Structure Type MOL
InChI Key FMNIEHIAIMPDIG-ZTKZIYFRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

630.8
MW (Da)
7.10
ALogP
8
HBA
1
HBD
95.6
PSA (Ų)
0.13
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 C37H46N2O7
MW 630.78
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.45

Activity Summary

IC50 2 meas. best 5.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.31 5.31 4940.0 1
Cholinesterase
CHEMBL1914
IC50 4.07 4.07 84400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 4940.0 nM 5.31 Inhibition of recombinant human AChE 15974596
Cholinesterase IC50 = 84400.0 nM 4.07 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

Data from ChEMBL 36 via Core Engine