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Compound Detail

CHEMBL264027

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CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1.O=C(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL264027
Phase Preclinical
Structure Type MOL
InChI Key UINLBFIPJXSKON-UHFFFAOYSA-N
Parent Compound CHEMBL26715
Active Moiety CHEMBL26715
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

306.4
MW (Da)
1.85
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.84
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H28N2O7
MW 396.44
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -0.62

Activity Summary

IC50 4 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 7.4 7.4 40.0 1
D(2) dopamine receptor
CHEMBL3998
IC50 6.22 6.22 600.0 1
Alpha-2A adrenergic receptor
CHEMBL4744
IC50 5.0 5.0 10000.0 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 4.22 4.22 60000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7912735 10.1021/jm00038a007 5-hydroxytryptamine receptor 1A 1
7912735 10.1021/jm00038a007 5-hydroxytryptamine receptor 1B 1
7912735 10.1021/jm00038a007 5-hydroxytryptamine receptor 2A 1
7912735 10.1021/jm00038a007 D(1A) dopamine receptor 1
7912735 10.1021/jm00038a007 D(2) dopamine receptor 1
7912735 10.1021/jm00038a007 Alpha-1A adrenergic receptor 1
7912735 10.1021/jm00038a007 Alpha-2A adrenergic receptor 1

Data from ChEMBL 36 via Core Engine