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Compound Detail

CHEMBL285777

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COc1ccc2[nH]cc(C3=CCN(C)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL285777
Phase Preclinical
Structure Type MOL
InChI Key TTZUYLGBEOWNTP-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

242.3
MW (Da)
2.90
ALogP
2
HBA
1
HBD
28.3
PSA (Ų)
0.88
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 -0.18

Activity Summary

Ki 3 meas. best 7.68
IC50 1 meas. best 6.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.68 7.68 20.9 2
Sodium-dependent serotonin transporter
CHEMBL228
IC50 6.14 6.14 730.0 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
Ki 6.05 6.05 897.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8258822 10.1021/jm00077a003 5-hydroxytryptamine receptor 1A 1
8258822 10.1021/jm00077a003 Serotonin 2 (5-HT2) receptor 1
8568799 10.1021/jm950410b 5-hydroxytryptamine receptor 1A 1
17391962 10.1016/j.bmcl.2007.03.040 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine