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Compound Detail

CHEMBL108532

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Nc1cccc(C#CCCN2CC=C(c3ccccc3)CC2)c1

Basic Information

ChEMBL ID CHEMBL108532
Phase Preclinical
Structure Type MOL
InChI Key KHTVRVDYYAMNRK-UHFFFAOYSA-N
5
Targets
7
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

302.4
MW (Da)
3.80
ALogP
2
HBA
1
HBD
29.3
PSA (Ų)
0.69
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N2
MW 302.42
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.52

Activity Summary

Ki 6 meas. best 9.44
EC50 1 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 9.44 9.44 0.4 1
D(2) dopamine receptor
CHEMBL217
EC50 8.01 8.01 9.8 1
D(2) dopamine receptor
CHEMBL339
Ki 7.75 7.29 18.0 3
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.97 6.97 107.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 5.81 5.81 1547.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8759640 10.1021/jm950721m D(2) dopamine receptor 4
8759640 10.1021/jm950721m Rattus norvegicus 3
8759640 10.1021/jm950721m Mus musculus 1
8759640 10.1021/jm950721m D(3) dopamine receptor 1
8759640 10.1021/jm950721m 5-hydroxytryptamine receptor 1A 1
8759640 10.1021/jm950721m Adrenergic receptor alpha-1 1
8759640 10.1021/jm950721m Monkey 1
15808487 10.1016/j.bmcl.2005.02.012 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine