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Compound Detail

CHEMBL273680

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c1ccc(CNc2nn3c(-c4ccccc4)nnc3c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL273680
Phase Preclinical
Structure Type MOL
InChI Key BGZRYVWWMJHNHC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
4.56
ALogP
5
HBA
1
HBD
55.1
PSA (Ų)
0.52
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 C22H17N5
MW 351.41
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.37

Activity Summary

Ki 1 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 6.61 6.61 243.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2836588 10.1021/jm00401a010 Mus musculus 2
15027873 10.1021/jm031020p GABA-A receptor; alpha-1/beta-3/gamma-2 1
15027873 10.1021/jm031020p GABA-A receptor; alpha-2/beta-3/gamma-2 1
15027873 10.1021/jm031020p GABA-A receptor; alpha-3/beta-3/gamma-2 1
15027873 10.1021/jm031020p GABA-A receptor; alpha-5/beta-3/gamma-2 1
2836588 10.1021/jm00401a010 GABA-A receptor; anion channel 1
2836588 10.1021/jm00401a010 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine