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Compound Detail

CHEMBL431973

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c1ccc(COc2ccc3c(c2)[nH]c2c4c5ccccc5nc-4c[nH]c23)cc1

Basic Information

ChEMBL ID CHEMBL431973
Phase Preclinical
Structure Type MOL
InChI Key LEGPDWOWUFGLMP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
5.88
ALogP
2
HBA
2
HBD
53.7
PSA (Ų)
0.41
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17N3O
MW 363.42
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.41

Activity Summary

Ki 3 meas. best 6.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 6.37 6.37 432.0 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 5.52 5.52 3000.0 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10633039 10.1021/jm990341r GABA-A receptor; alpha-1/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-2/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-3/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-5/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-6/beta-3/gamma-2 1
2167978 10.1021/jm00171a015 GABA-A receptor; anion channel 1

Data from ChEMBL 36 via Core Engine