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Compound Detail

CHEMBL4862839

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COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2

Basic Information

ChEMBL ID CHEMBL4862839
Phase Preclinical
Structure Type MOL
InChI Key LTNOCTARMCCZMF-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
5.20
ALogP
4
HBA
2
HBD
61.8
PSA (Ų)
0.52
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24Cl2N2O3
MW 471.38
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.06

Activity Summary

Ki 4 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 6.55 6.55 280.0 1
D(3) dopamine receptor
CHEMBL234
Ki 6.34 6.34 460.0 1
Sigma intracellular receptor 2
CHEMBL4105907
Ki 6.32 6.32 480.0 1
D(4) dopamine receptor
CHEMBL219
Ki 5.94 5.94 1150.0 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