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Compound Detail

CHEMBL543603

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Br.CCCCCCc1c(O)noc1C1CCNCC1

Basic Information

ChEMBL ID CHEMBL543603
Phase Preclinical
Structure Type MOL
InChI Key GKEZEXQIUIXYNR-UHFFFAOYSA-N
Parent Compound CHEMBL1192379
Active Moiety CHEMBL1192379
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

252.4
MW (Da)
2.97
ALogP
4
HBA
2
HBD
58.3
PSA (Ų)
0.76
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H25BrN2O2
MW 333.27
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness 0.37

Activity Summary

IC50 1 meas. best 5.96
Ki 1 meas. best 5.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mus musculus
CHEMBL375
IC50 5.96 5.96 1100.0 1
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.35 5.35 4500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12036354 10.1021/jm020027o GABA-A receptor; anion channel 1
12036354 10.1021/jm020027o Gamma-aminobutyric acid type B receptor subunit 1 1
12036354 10.1021/jm020027o Mus musculus 1

Data from ChEMBL 36 via Core Engine