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Compound Detail

CHEMBL11787

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O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2c(ccc3ccccc23)O1

Basic Information

ChEMBL ID CHEMBL11787
Phase Preclinical
Structure Type MOL
InChI Key CPZXZWSBPRKTEA-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

436.6
MW (Da)
4.06
ALogP
5
HBA
1
HBD
67.9
PSA (Ų)
0.52
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 C26H32N2O4
MW 436.55
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.01

Activity Summary

IC50 5 meas. best 6.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL339
IC50 6.5 6.5 316.2 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 6.1 6.1 794.3 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 5.9 5.9 1258.9 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 5.5 5.5 3162.3 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 5.2 5.2 6309.6 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