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Compound Detail

CHEMBL394710

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C#Cc1ccc2c(c1)c(=O)n(C)c1c(C(=O)OCCOC(=O)c3ncn4c5ccc(C#C)cc5c(=O)n(C)c34)ncn21

Basic Information

ChEMBL ID CHEMBL394710
Phase Preclinical
Structure Type MOL
InChI Key HQCFOKBDGJUVDT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

560.5
MW (Da)
1.66
ALogP
12
HBA
0
HBD
131.2
PSA (Ų)
0.18
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H20N6O6
MW 560.53
Aromatic Rings 6
Heavy Atoms 42
NP-Likeness -0.67

Activity Summary

Ki 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 7.82 7.82 15.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; alpha-5/beta-3/gamma-2 Ki = 15.0 nM 7.82 Binding affinity to GABAA alpha-5-beta-3-gamma-2 receptor 18537233

Literature References

PubMed DOI Target Context # Activities
18537233 10.1021/jm701433b Unchecked 5
18537233 10.1021/jm701433b GABA-A receptor; alpha-6/beta-3/gamma-2 2
18537233 10.1021/jm701433b GABA A receptor alpha-4/beta-3/gamma-2 2
18537233 10.1021/jm701433b Gamma-aminobutyric acid receptor subunit alpha-5 1
18537233 10.1021/jm701433b Mus musculus 1
18537233 10.1021/jm701433b GABA-A receptor; alpha-2/beta-3/gamma-2 1
18537233 10.1021/jm701433b GABA-A receptor; alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine