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Compound Detail

CHEMBL3144697

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O=c1c2cnc3ccc(Br)cc3c2[nH]n1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL3144697
Phase Preclinical
Structure Type MOL
InChI Key QZWILCKFBLOODV-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

340.2
MW (Da)
3.63
ALogP
3
HBA
1
HBD
50.7
PSA (Ų)
0.58
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H10BrN3O
MW 340.18
Aromatic Rings 4
Heavy Atoms 21
NP-Likeness -1.14

Activity Summary

Ki 5 meas. best 10.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 10.3 10.3 0.1 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 10.22 10.22 0.1 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 10.1 10.1 0.1 1
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 9.92 9.92 0.1 1
GABA-A receptor; alpha-6/beta-3/gamma-2
CHEMBL2095190
Ki 8.4 8.4 4.0 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

Data from ChEMBL 36 via Core Engine