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Compound Detail

CHEMBL2403793

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COc1ccc(C(/C=C/CNC(C)CC(=O)O)(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1

Basic Information

ChEMBL ID CHEMBL2403793
Phase Preclinical
Structure Type MOL
InChI Key XLQATTZTRJREOA-BLLMUTORSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
5.06
ALogP
5
HBA
2
HBD
77.0
PSA (Ų)
0.28
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33NO5
MW 475.59
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.02

Activity Summary

IC50 2 meas. best 4.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter 4
CHEMBL3699
IC50 4.22 4.22 60256.0 1
GABA transporter 3
CHEMBL5205
IC50 4.2 4.2 63095.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23770450 10.1016/j.ejmech.2013.04.063 GABA transporter 2 1
23770450 10.1016/j.ejmech.2013.04.063 Sodium- and chloride-dependent GABA transporter 1 1
23770450 10.1016/j.ejmech.2013.04.063 GABA transporter 4 1
23770450 10.1016/j.ejmech.2013.04.063 GABA transporter 3 1

Data from ChEMBL 36 via Core Engine