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Compound Detail

CHEMBL1814307

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CCCc1cc(N)c(O)c(-c2ccc(OC)c(CCC)c2)c1

Basic Information

ChEMBL ID CHEMBL1814307
Phase Preclinical
Structure Type MOL
InChI Key CORBPQMJMWUNPD-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

299.4
MW (Da)
4.56
ALogP
3
HBA
2
HBD
55.5
PSA (Ų)
0.61
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H25NO2
MW 299.41
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.33

Activity Summary

EC50 4 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
CHEMBL3885571
EC50 5.5 5.5 3200.0 1
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2
CHEMBL3885576
EC50 5.28 5.28 5300.0 1
Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2
CHEMBL3885572
EC50 5.08 5.08 8400.0 1
GABA-A receptor; GABA-A site (alpha1/beta2 interface)
CHEMBL1907597
EC50 5.04 5.04 9200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21699169 10.1021/jm200186n GABA-A receptor; GABA-A site (alpha1/beta2 interface) 3
21699169 10.1021/jm200186n Gamma-aminobutyric acid receptor subunit alpha-5/beta-2 2
21699169 10.1021/jm200186n Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2 2
21699169 10.1021/jm200186n Gamma-aminobutyric acid receptor subunit alpha-2/beta-2 2
21699169 10.1021/jm200186n No relevant target 1

Data from ChEMBL 36 via Core Engine