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Compound Detail

CHEMBL2178791

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COc1ccc2c3c1O[C@H]1C[C@@H](O)C=C[C@@]31CCN(CCOCCOCCNC13CC4CC(C)(CC(C)(C4)C1)C3)C2

Basic Information

ChEMBL ID CHEMBL2178791
Phase Preclinical
Structure Type MOL
InChI Key NWTKQFTXRMPAJC-WDOOIYNRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

566.8
MW (Da)
4.59
ALogP
7
HBA
2
HBD
72.4
PSA (Ų)
0.30
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H50N2O5
MW 566.78
Aromatic Rings 1
Heavy Atoms 41
NP-Likeness 0.61

Activity Summary

IC50 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL3199
IC50 7.09 7.09 80.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 80.9 nM 7.09 Inhibition of AChE in Wistar rat brain homogenates using acetylthiocholine iodid... 23033965

Literature References

PubMed DOI Target Context # Activities
23033965 10.1021/jm3009458 SH-SY5Y 1
23033965 10.1021/jm3009458 Glutamate receptor ionotropic, NMDA 2B 1
23033965 10.1021/jm3009458 Unchecked 1
23033965 10.1021/jm3009458 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine