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Compound Detail

CHEMBL545694

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Cl.O=C(O)[C@@H]1CCCN(CCOCCN2c3cc(Cl)ccc3CCc3ccc(Cl)cc32)C1

Basic Information

ChEMBL ID CHEMBL545694
Phase Preclinical
Structure Type MOL
InChI Key PMTZTCZFJYDWAV-FSRHSHDFSA-N
Parent Compound CHEMBL1194169
Active Moiety CHEMBL1194169
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

463.4
MW (Da)
5.04
ALogP
4
HBA
1
HBD
53.0
PSA (Ų)
0.58
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29Cl3N2O3
MW 499.87
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.92

Activity Summary

IC50 1 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA transporter
CHEMBL2111478
IC50 7.17 7.17 68.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA transporter IC50 = 68.0 nM 7.17 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