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Compound Detail

CHEMBL4633772

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C#CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2

Basic Information

ChEMBL ID CHEMBL4633772
Phase Preclinical
Structure Type MOL
InChI Key SBQXZROAPGSYPJ-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
3.42
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N2O3
MW 376.46
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness 0.24

Activity Summary

Ki 6 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
Ki 7.24 7.24 58.0 2
D(2) dopamine receptor
CHEMBL217
Ki 6.07 6.07 854.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.9 5.9 1272.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32107165 10.1016/j.bmcl.2020.127053 ADMET 5
32107165 10.1016/j.bmcl.2020.127053 D(2) dopamine receptor 1
32107165 10.1016/j.bmcl.2020.127053 D(1A) dopamine receptor 1
32107165 10.1016/j.bmcl.2020.127053 5-hydroxytryptamine receptor 2A 1
32107165 10.1016/j.bmcl.2020.127053 5-hydroxytryptamine receptor 1A 1
32107165 10.1016/j.bmcl.2020.127053 D(1B) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 D(1A) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 D(2) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 5-hydroxytryptamine receptor 2A 1

Data from ChEMBL 36 via Core Engine