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Compound Detail

CHEMBL4794776

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Cc1ccsc1C(=CCCN(C)C(CCO)C(=O)NCc1ccccc1Cl)c1sccc1C

Basic Information

ChEMBL ID CHEMBL4794776
Phase Preclinical
Structure Type MOL
InChI Key IJIMBHRRVMFBCK-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

503.1
MW (Da)
5.90
ALogP
5
HBA
2
HBD
52.6
PSA (Ų)
0.34
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H31ClN2O2S2
MW 503.13
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.78

Activity Summary

IC50 4 meas. best 5.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter 4
CHEMBL3699
IC50 5.31 5.275 4897.8 2
GABA transporter 3
CHEMBL5205
IC50 4.98 4.98 10471.3 1
Sodium- and chloride-dependent GABA transporter 1
CHEMBL5445
IC50 4.86 4.86 13803.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31901745 10.1016/j.ejmech.2019.111920 Mus musculus 13
31901745 10.1016/j.ejmech.2019.111920 GABA transporter 4 2
31901745 10.1016/j.ejmech.2019.111920 Sodium- and chloride-dependent GABA transporter 1 2
31901745 10.1016/j.ejmech.2019.111920 GABA transporter 3 1
31901745 10.1016/j.ejmech.2019.111920 No relevant target 1

Data from ChEMBL 36 via Core Engine