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Compound Detail

CHEMBL544301

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Br.Oc1noc(C2CCNCC2)c1Cc1ccc(-c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL544301
Phase Preclinical
Structure Type MOL
InChI Key QIHPJFBAKAZCCA-UHFFFAOYSA-N
Parent Compound CHEMBL1192976
Active Moiety CHEMBL1192976
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
4.11
ALogP
4
HBA
2
HBD
58.3
PSA (Ų)
0.75
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23BrN2O2
MW 415.33
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.05

Activity Summary

IC50 1 meas. best 6.15
Ki 1 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 6.4 6.4 400.0 1
Mus musculus
CHEMBL375
IC50 6.15 6.15 710.0 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