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Compound Detail

CHEMBL4566905

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O=C1Nc2ccc(-c3cccs3)cc2C1=O

Basic Information

ChEMBL ID CHEMBL4566905
Phase Preclinical
Structure Type MOL
InChI Key YOFGZEWPLABWQJ-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

229.3
MW (Da)
2.55
ALogP
3
HBA
1
HBD
46.2
PSA (Ų)
0.76
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H7NO2S
MW 229.26
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -0.88

Activity Summary

IC50 6 meas. best 5.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter 4
CHEMBL3699
IC50 5.2 4.905 6309.6 2
Sodium- and chloride-dependent GABA transporter 3
CHEMBL5208
IC50 5.09 5.09 8128.3 1
Sodium- and chloride-dependent GABA transporter 1
CHEMBL5445
IC50 4.53 4.53 29512.1 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 3 2
30503411 10.1016/j.bmc.2018.11.028 Sodium- and chloride-dependent GABA transporter 3 1
30503411 10.1016/j.bmc.2018.11.028 GABA transporter 4 1
30503411 10.1016/j.bmc.2018.11.028 GABA transporter 3 1
30503411 10.1016/j.bmc.2018.11.028 GABA transporter 2 1
30503411 10.1016/j.bmc.2018.11.028 Sodium- and chloride-dependent GABA transporter 1 1
31901745 10.1016/j.ejmech.2019.111920 Sodium- and chloride-dependent GABA transporter 1 1
31901745 10.1016/j.ejmech.2019.111920 GABA transporter 4 1

Data from ChEMBL 36 via Core Engine