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Compound Detail

CHEMBL382005

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CC(C)(O)c1ccn2c(-c3ccc(F)c(-c4ncc(F)cc4F)c3)cnc2n1

Basic Information

ChEMBL ID CHEMBL382005
Phase Preclinical
Structure Type MOL
InChI Key UVTIJQDSGQQUDX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
4.10
ALogP
5
HBA
1
HBD
63.3
PSA (Ų)
0.58
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15F3N4O
MW 384.36
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.97

Activity Summary

Ki 3 meas. best 8.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 8.95 8.95 1.1 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 8.75 8.75 1.8 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 8.43 8.43 3.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-1/beta-3/gamma-2 2
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-3/beta-3/gamma-2 2
16386900 10.1016/j.bmcl.2005.12.044 GABA-A receptor; alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine