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Compound Detail

CHEMBL74302

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O=C(NCc1ccc([N+](=O)[O-])cc1)C(=O)c1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL74302
Phase Preclinical
Structure Type MOL
InChI Key SQVFGSDZEHNBTN-UHFFFAOYSA-N
6
Targets
8
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

323.3
MW (Da)
2.58
ALogP
4
HBA
2
HBD
105.1
PSA (Ų)
0.33
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 C17H13N3O4
MW 323.31
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.10

Activity Summary

Ki 8 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095167
Ki 7.8 7.8 16.0 2
GABA-A receptor; anion channel
CHEMBL2094107
Ki 7.68 7.68 21.0 1
Unchecked
CHEMBL612545
Ki 7.68 7.68 21.0 1
GABA A receptor alpha-5/beta-3/gamma-2
CHEMBL2111374
Ki 7.24 7.24 58.0 2
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL341
Ki 6.68 6.68 210.0 1
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111343
Ki 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11428922 10.1021/jm010827j GABA-A receptor; anion channel 5
11428922 10.1021/jm010827j GABA-A receptor; alpha-1/beta-2/gamma-2 1
11428922 10.1021/jm010827j GABA A receptor alpha-3/beta-2/gamma-2 1
11428922 10.1021/jm010827j GABA A receptor alpha-5/beta-3/gamma-2 1
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