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Compound Detail

CHEMBL433741

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COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1

Basic Information

ChEMBL ID CHEMBL433741
Phase Preclinical
Structure Type MOL
InChI Key HDEPBPKSVYTTAM-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

395.6
MW (Da)
3.64
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.69
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33N3O2
MW 395.55
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.52

Activity Summary

Ki 5 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL3138
Ki 9.77 9.77 0.2 1
D(4) dopamine receptor
CHEMBL219
Ki 7.2 7.2 63.6 1
D(2) dopamine receptor
CHEMBL217
Ki 7.11 7.11 77.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.57 6.57 268.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.14 6.14 717.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12477356 10.1021/jm020952a D(3) dopamine receptor 1
12477356 10.1021/jm020952a D(4) dopamine receptor 1
12477356 10.1021/jm020952a D(2) dopamine receptor 1
12477356 10.1021/jm020952a 5-hydroxytryptamine receptor 1A 1
12477356 10.1021/jm020952a Adrenergic receptor alpha-1 1
12477356 10.1021/jm020952a No relevant target 1

Data from ChEMBL 36 via Core Engine