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Compound Detail

CHEMBL48211

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Cc1cccc2c1N(C(=O)N1CCOCC1)Cc1c(-c3noc(C4CC4)n3)ncn1-2

Basic Information

ChEMBL ID CHEMBL48211
Phase Preclinical
Structure Type MOL
InChI Key BIBRQTYVULTGSH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
2.88
ALogP
7
HBA
0
HBD
89.5
PSA (Ų)
0.65
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 C21H22N6O3
MW 406.45
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.66

Activity Summary

Ki 3 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 8.34 8.34 4.6 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
Ki 8.33 8.33 4.7 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111339
Ki 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8568803 10.1021/jm940765f GABA-A receptor; anion channel 2
8568803 10.1021/jm940765f Rattus norvegicus 2
8568803 10.1021/jm940765f GABA-A receptor; alpha-1/beta-2/gamma-2 1
8568803 10.1021/jm940765f GABA A receptor alpha-3/beta-2/gamma-2 1
8568803 10.1021/jm940765f GABA A receptor alpha-6/beta-2/gamma-2 1

Data from ChEMBL 36 via Core Engine