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Compound Detail

CHEMBL4863748

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COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2

Basic Information

ChEMBL ID CHEMBL4863748
Phase Preclinical
Structure Type MOL
InChI Key AIYKVNCJQXICKY-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

436.9
MW (Da)
4.54
ALogP
4
HBA
2
HBD
61.8
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25ClN2O3
MW 436.94
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.07

Activity Summary

Ki 4 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 6.72 6.72 190.0 1
D(3) dopamine receptor
CHEMBL234
Ki 6.42 6.42 380.0 1
Sigma intracellular receptor 2
CHEMBL4105907
Ki 6.36 6.36 440.0 1
D(4) dopamine receptor
CHEMBL219
Ki 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33882273 10.1016/j.bmcl.2021.128047 D(1A) dopamine receptor 1
33882273 10.1016/j.bmcl.2021.128047 D(1B) dopamine receptor 1
33882273 10.1016/j.bmcl.2021.128047 D(2) dopamine receptor 1
33882273 10.1016/j.bmcl.2021.128047 D(3) dopamine receptor 1
33882273 10.1016/j.bmcl.2021.128047 D(4) dopamine receptor 1
33882273 10.1016/j.bmcl.2021.128047 Sigma intracellular receptor 2 1

Data from ChEMBL 36 via Core Engine