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Compound Detail

CHEMBL4577162

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CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC.Cl

Basic Information

ChEMBL ID CHEMBL4577162
Phase Preclinical
Structure Type MOL
InChI Key XQXLIZUFYLRIQF-UHFFFAOYSA-N
Parent Compound CHEMBL4595382
Active Moiety CHEMBL4595382
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

468.0
MW (Da)
5.86
ALogP
3
HBA
2
HBD
57.4
PSA (Ų)
0.33
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35Cl2N3O2
MW 504.50
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.79

Activity Summary

Ki 6 meas. best 7.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.94 7.94 11.5 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 7.07 7.07 85.1 1
D(4) dopamine receptor
CHEMBL219
Ki 6.24 6.24 575.0 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.09 6.09 818.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.85 5.85 1421.0 1
D(1B) dopamine receptor
CHEMBL1850
Ki 5.37 5.37 4227.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32282200 10.1021/acs.jmedchem.9b01835 D(1A) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(2) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(3) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(4) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 D(1B) dopamine receptor 1
32282200 10.1021/acs.jmedchem.9b01835 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine