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Compound Detail

CHEMBL175475

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COCCOc1cccnc1COc1nn2c(-c3ccccc3)nnc2c2c1C1CCC2CC1

Basic Information

ChEMBL ID CHEMBL175475
Phase Preclinical
Structure Type MOL
InChI Key QGOAGGOYLMIFPI-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
4.55
ALogP
8
HBA
0
HBD
83.7
PSA (Ų)
0.36
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N5O3
MW 457.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.09

Activity Summary

Ki 4 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 9.3 9.3 0.5 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 8.41 8.41 3.9 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 8.01 8.01 9.8 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 7.89 7.89 13.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15743180 10.1021/jm040883v GABA-A receptor; alpha-1/beta-3/gamma-2 2
15743180 10.1021/jm040883v GABA-A receptor; alpha-3/beta-3/gamma-2 2
15743180 10.1021/jm040883v GABA-A receptor; alpha-2/beta-3/gamma-2 1
15743180 10.1021/jm040883v GABA-A receptor; alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine