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Compound Detail

CHEMBL12124

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O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@@H]1COc2ccccc2O1

Basic Information

ChEMBL ID CHEMBL12124
Phase Preclinical
Structure Type MOL
InChI Key HCVRCHQFYYZPHT-QGZVFWFLSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

386.5
MW (Da)
2.91
ALogP
5
HBA
1
HBD
67.9
PSA (Ų)
0.58
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 C22H30N2O4
MW 386.49
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.24

Activity Summary

IC50 6 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 7.7 7.7 19.9 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 7.2 7.2 63.1 1
Adrenergic receptor alpha-2
CHEMBL2093864
IC50 6.2 6.2 631.0 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 6.1 6.1 794.3 1
D(2) dopamine receptor
CHEMBL339
IC50 5.6 5.6 2511.9 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3373482 10.1021/jm00401a007 5-hydroxytryptamine receptor 1A 1
3373482 10.1021/jm00401a007 5-hydroxytryptamine receptor 1B 1
3373482 10.1021/jm00401a007 Serotonin 2 (5-HT2) receptor 1
3373482 10.1021/jm00401a007 Adrenergic receptor alpha-1 1
3373482 10.1021/jm00401a007 Adrenergic receptor alpha-2 1
3373482 10.1021/jm00401a007 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine