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Compound Detail

CHEMBL1773937

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Cl.O=C(O)CCc1ncc[nH]1

Basic Information

ChEMBL ID CHEMBL1773937
Phase Preclinical
Structure Type MOL
InChI Key FNFOMFMVOHBKHO-UHFFFAOYSA-N
Parent Compound CHEMBL1789770
Active Moiety CHEMBL1789770
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

140.1
MW (Da)
0.43
ALogP
2
HBA
2
HBD
66.0
PSA (Ų)
0.64
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C6H9ClN2O2
MW 176.60
Aromatic Rings 1
Heavy Atoms 10
NP-Likeness -0.94

Activity Summary

IC50 3 meas. best 4.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter 4
CHEMBL3699
IC50 4.54 4.54 28840.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA transporter 4 IC50 = 28840.32 nM 4.54 Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells 21353350

Literature References

PubMed DOI Target Context # Activities
21353350 10.1016/j.ejmech.2011.01.042 Unchecked 4
21353350 10.1016/j.ejmech.2011.01.042 Sodium- and chloride-dependent GABA transporter 1 1
21353350 10.1016/j.ejmech.2011.01.042 GABA transporter 3 1
21353350 10.1016/j.ejmech.2011.01.042 GABA transporter 4 1

Data from ChEMBL 36 via Core Engine