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Compound Detail

CHEMBL543108

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Cl.O=C(O)[C@@H]1CCCN(CCOCCN2c3ccccc3CCc3ccc(Cl)cc32)C1

Basic Information

ChEMBL ID CHEMBL543108
Phase Preclinical
Structure Type MOL
InChI Key DONMADPWKKWSOE-VEIFNGETSA-N
Parent Compound CHEMBL1191940
Active Moiety CHEMBL1191940
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

429.0
MW (Da)
4.39
ALogP
4
HBA
1
HBD
53.0
PSA (Ų)
0.66
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30Cl2N2O3
MW 465.42
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.05

Activity Summary

IC50 1 meas. best 7.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter
CHEMBL2111478
IC50 7.13 7.13 74.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA transporter IC50 = 74.0 nM 7.13 In vitro inhibition of [3H]GABA uptake in rat synaptosomes was determined 11405652

Literature References

PubMed DOI Target Context # Activities
11405652 10.1021/jm990513k GABA transporter 4

Data from ChEMBL 36 via Core Engine