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Compound Detail

CHEMBL156845

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COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1

Basic Information

ChEMBL ID CHEMBL156845
Phase Preclinical
Structure Type MOL
InChI Key LTPWRNUOYXUBGY-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

353.5
MW (Da)
2.56
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.87
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27N3O2
MW 353.47
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.77

Activity Summary

Ki 5 meas. best 10.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 10.6 10.6 0.0 1
D(4) dopamine receptor
CHEMBL3361
Ki 8.04 8.04 9.2 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.37 6.37 432.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.34 6.34 454.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.13 5.13 7460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20873719 10.1021/jm100925m No relevant target 3
12477356 10.1021/jm020952a D(3) dopamine receptor 2
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
20873719 10.1021/jm100925m D(4) dopamine receptor 1
20873719 10.1021/jm100925m D(2) dopamine receptor 1
20873719 10.1021/jm100925m Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine