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Compound Detail

CHEMBL3290191

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O=C1/C(=C\c2ccc(N3CCCC3)cc2)CN(Cc2ccccc2)C/C1=C\c1ccc(N2CCCC2)cc1

Basic Information

ChEMBL ID CHEMBL3290191
Phase Preclinical
Structure Type MOL
InChI Key RRMYFAUOOIISIJ-KURJDURESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

503.7
MW (Da)
6.44
ALogP
4
HBA
0
HBD
26.8
PSA (Ų)
0.36
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H37N3O
MW 503.69
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.67

Activity Summary

IC50 1 meas. best 4.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 4.25 4.25 56920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 56920.0 nM 4.25 Inhibition of BuChE (unknown origin) after 5 mins by Ellman's method 24980117

Literature References

PubMed DOI Target Context # Activities
24980117 10.1016/j.ejmech.2014.06.034 Radical scavenging activity 1
24980117 10.1016/j.ejmech.2014.06.034 ADMET 1
24980117 10.1016/j.ejmech.2014.06.034 NON-PROTEIN TARGET 1
24980117 10.1016/j.ejmech.2014.06.034 Acetylcholinesterase 1
24980117 10.1016/j.ejmech.2014.06.034 Cholinesterase 1

Data from ChEMBL 36 via Core Engine