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Compound Detail

CHEMBL81191

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NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccccc23)CC1

Basic Information

ChEMBL ID CHEMBL81191
Phase Preclinical
Structure Type MOL
InChI Key JNYHVVZVSHDECL-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

412.5
MW (Da)
4.73
ALogP
3
HBA
1
HBD
55.6
PSA (Ų)
0.66
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28N2O2
MW 412.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.49

Activity Summary

Ki 5 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 8.49 8.49 3.2 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 8.27 8.27 5.4 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 6.82 6.82 153.0 1
D(2) dopamine receptor
CHEMBL339
Ki 6.78 6.78 167.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.65 6.65 224.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15109634 10.1016/j.bmcl.2004.03.003 5-hydroxytryptamine receptor 1D 1
15109634 10.1016/j.bmcl.2004.03.003 5-hydroxytryptamine receptor 1B 1
15109634 10.1016/j.bmcl.2004.03.003 Sodium-dependent serotonin transporter 1
15109634 10.1016/j.bmcl.2004.03.003 Adrenergic receptor alpha-1 1
15109634 10.1016/j.bmcl.2004.03.003 D(2) dopamine receptor 1
15109634 10.1016/j.bmcl.2004.03.003 Cavia porcellus 1

Data from ChEMBL 36 via Core Engine