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Compound Detail

CHEMBL10597

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CCOC(=O)c1cc2c3cc(OCc4ccccc4)ccc3nc-2c[nH]1

Basic Information

ChEMBL ID CHEMBL10597
Phase Preclinical
Structure Type MOL
InChI Key UKGVLKDJTMUFNB-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
4.42
ALogP
4
HBA
1
HBD
64.2
PSA (Ų)
0.54
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 C21H18N2O3
MW 346.39
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.67

Activity Summary

Ki 4 meas. best 8.14
IC50 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 8.14 8.14 7.2 1
GABA-A receptor; anion channel
CHEMBL1907607
IC50 8.05 8.05 8.9 1
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 6.77 6.77 169.0 1
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 6.57 6.57 271.0 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 6.55 6.55 284.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10633039 10.1021/jm990341r GABA-A receptor; alpha-1/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-2/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-3/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-5/beta-3/gamma-2 1
10633039 10.1021/jm990341r GABA-A receptor; alpha-6/beta-3/gamma-2 1
1968513 10.1021/jm00165a028 GABA-A receptor; anion channel 1
1968513 10.1021/jm00165a028 Mus musculus 1

Data from ChEMBL 36 via Core Engine