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Compound Detail

CHEMBL4095588

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COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1.Cl

Basic Information

ChEMBL ID CHEMBL4095588
Phase Preclinical
Structure Type MOL
InChI Key VAYHWGJKUOSHOE-UHFFFAOYSA-N
Parent Compound CHEMBL4116454
Active Moiety CHEMBL4116454
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

445.6
MW (Da)
4.66
ALogP
5
HBA
1
HBD
54.0
PSA (Ų)
0.51
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32ClN3O3
MW 482.02
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.10

Activity Summary

EC50 1 meas. best 7.85
IC50 1 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fatty-acid amide hydrolase 1
CHEMBL2243
IC50 8.59 8.59 2.6 1
D(3) dopamine receptor
CHEMBL234
EC50 7.85 7.85 14.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28182408 10.1021/acs.jmedchem.6b01578 D(3) dopamine receptor 2
28182408 10.1021/acs.jmedchem.6b01578 Fatty-acid amide hydrolase 1 1

Data from ChEMBL 36 via Core Engine