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Compound Detail

CHEMBL4787153

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Cc1ccsc1C(=CCCN(C)C1CCc2onc(O)c2C1)c1sccc1C

Basic Information

ChEMBL ID CHEMBL4787153
Phase Preclinical
Structure Type MOL
InChI Key ZFGNKGXSCJMQFX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

414.6
MW (Da)
5.43
ALogP
6
HBA
1
HBD
49.5
PSA (Ų)
0.58
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N2O2S2
MW 414.60
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.71

Activity Summary

IC50 2 meas. best 5.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium- and chloride-dependent GABA transporter 1
CHEMBL5445
IC50 5.15 5.15 7079.5 1
GABA transporter 3
CHEMBL5205
IC50 4.59 4.59 25704.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31901745 10.1016/j.ejmech.2019.111920 GABA transporter 4 2
31901745 10.1016/j.ejmech.2019.111920 GABA transporter 3 1
31901745 10.1016/j.ejmech.2019.111920 Sodium- and chloride-dependent GABA transporter 1 1

Data from ChEMBL 36 via Core Engine