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Compound Detail

CHEMBL5178760

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O=C(O)C1CCCN(CC/C=C/c2ccccc2-c2ccc(Cl)cc2Cl)C1

Basic Information

ChEMBL ID CHEMBL5178760
Phase Preclinical
Structure Type MOL
InChI Key QQNWSPUETZHQIX-XVNBXDOJSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

404.3
MW (Da)
5.86
ALogP
2
HBA
1
HBD
40.5
PSA (Ų)
0.66
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23Cl2NO2
MW 404.34
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.57

Activity Summary

IC50 1 meas. best 7.28
Ki 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium- and chloride-dependent GABA transporter 1
CHEMBL5445
Ki 8.05 8.05 8.9 1
Sodium- and chloride-dependent GABA transporter 1
CHEMBL5445
IC50 7.28 7.28 52.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35306287 10.1016/j.ejmech.2022.114269 Sodium- and chloride-dependent GABA transporter 1 2

Data from ChEMBL 36 via Core Engine