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Compound Detail

CHEMBL495635

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COc1ccc2c(c1)CCC2NC(=O)C(=O)c1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL495635
Phase Preclinical
Structure Type MOL
InChI Key FKIFCJXVYFACJA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
3.16
ALogP
3
HBA
2
HBD
71.2
PSA (Ų)
0.57
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H18N2O3
MW 334.38
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.35

Activity Summary

Ki 3 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095167
Ki 6.61 6.61 246.0 1
Unchecked
CHEMBL612545
Ki 6.2 6.2 636.0 1
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL341
Ki 6.16 6.16 690.0 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