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Compound Detail

CHEMBL4877460

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COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2

Basic Information

ChEMBL ID CHEMBL4877460
Phase Preclinical
Structure Type MOL
InChI Key XFLGSSQRQNMLNA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
3.76
ALogP
5
HBA
2
HBD
85.6
PSA (Ų)
0.63
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 C26H25N3O3
MW 427.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.17

Activity Summary

Ki 3 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 7.58 7.58 26.0 1
D(2) dopamine receptor
CHEMBL217
Ki 7.41 7.41 39.0 1
D(4) dopamine receptor
CHEMBL219
Ki 5.47 5.47 3360.0 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