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Compound Detail

CHEMBL95020

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O=C1Cc2c(ccc3c(CCC4CCN(Cc5ccccc5)CC4)noc23)N1

Basic Information

ChEMBL ID CHEMBL95020
Phase Preclinical
Structure Type MOL
InChI Key OICRNZHKHYSUOP-UHFFFAOYSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

375.5
MW (Da)
4.17
ALogP
4
HBA
1
HBD
58.4
PSA (Ų)
0.73
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25N3O2
MW 375.47
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.73

Activity Summary

IC50 5 meas. best 8.44
Ki 1 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 8.44 8.44 3.6 4
Acetylcholinesterase
CHEMBL220
Ki 8.44 8.44 3.6 1
Cholinesterase
CHEMBL1914
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15481986 10.1021/jm049695v Acetylcholinesterase 2
7636841 10.1021/jm00015a002 Acetylcholinesterase 1
7636841 10.1021/jm00015a002 Cholinesterase 1
7636841 10.1021/jm00015a002 Unchecked 1
20053484 10.1016/j.ejmech.2009.12.038 Acetylcholinesterase 1
21074294 10.1016/j.ejmech.2010.10.009 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine