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Compound Detail

CHEMBL495634

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COc1ccc2c(c1)CCC2NC(=O)C(=O)c1c[nH]c2ccc([N+](=O)[O-])cc12

Basic Information

ChEMBL ID CHEMBL495634
Phase Preclinical
Structure Type MOL
InChI Key VDHLHILIXOHGNF-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

379.4
MW (Da)
3.07
ALogP
5
HBA
2
HBD
114.3
PSA (Ų)
0.31
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17N3O5
MW 379.37
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.74

Activity Summary

Ki 4 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.89 7.89 13.0 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095167
Ki 7.55 7.55 28.0 1
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL341
Ki 6.64 6.64 231.0 1
GABA A receptor alpha-5/beta-3/gamma-2
CHEMBL2111374
Ki 6.6 6.6 252.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19469479 10.1021/jm9001154 Unchecked 1
19469479 10.1021/jm9001154 GABA-A receptor; alpha-1/beta-2/gamma-2 1
19469479 10.1021/jm9001154 Gamma-aminobutyric acid receptor subunit alpha-2 1
19469479 10.1021/jm9001154 GABA A receptor alpha-5/beta-3/gamma-2 1

Data from ChEMBL 36 via Core Engine