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Compound Detail

CHEMBL543365

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Br.CCc1c(O)noc1C1CCNCC1

Basic Information

ChEMBL ID CHEMBL543365
Phase Preclinical
Structure Type MOL
InChI Key PTJZLQCGGWIPMN-UHFFFAOYSA-N
Parent Compound CHEMBL143993
Active Moiety CHEMBL143993
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

196.2
MW (Da)
1.41
ALogP
4
HBA
2
HBD
58.3
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H17BrN2O2
MW 277.16
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness 0.08

Activity Summary

IC50 1 meas. best 4.99
Ki 1 meas. best 5.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.2 5.2 6300.0 1
Mus musculus
CHEMBL375
IC50 4.99 4.99 10300.0 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