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Compound Detail

CHEMBL194305

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COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1

Basic Information

ChEMBL ID CHEMBL194305
Phase Preclinical
Structure Type MOL
InChI Key ZQZWLJUKYOXRPN-UHFFFAOYSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

242.3
MW (Da)
2.86
ALogP
2
HBA
2
HBD
37.0
PSA (Ų)
0.85
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18N2O
MW 242.32
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.09

Activity Summary

IC50 6 meas. best 7.1
EC50 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ADMET
CHEMBL612558
EC50 8.24 8.24 5.8 1
5-hydroxytryptamine receptor 6
CHEMBL3371
IC50 7.1 7.1 80.0 2
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 6.51 6.51 310.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 6.37 6.37 430.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
IC50 5.01 5.01 9800.0 1
5-hydroxytryptamine receptor 4
CHEMBL5017
IC50 5.01 5.01 9800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 6 3
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 4 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 7 1
16055331 10.1016/j.bmcl.2005.06.067 ADMET 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 1A 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 1B 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 1D 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 2A 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 2C 1
16055331 10.1016/j.bmcl.2005.06.067 5-hydroxytryptamine receptor 3A 1

Data from ChEMBL 36 via Core Engine