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Compound Detail

CHEMBL44533

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Cc1csc(-c2cc(-c3ccccc3)c3n(c2=O)CCCc2ccncc2-3)n1

Basic Information

ChEMBL ID CHEMBL44533
Phase Preclinical
Structure Type MOL
InChI Key NTQIDFIQUNKLIH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
4.96
ALogP
5
HBA
0
HBD
47.8
PSA (Ų)
0.49
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19N3OS
MW 385.49
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.03

Activity Summary

Ki 3 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL4956
Ki 9.52 9.52 0.3 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 9.4 9.4 0.4 1
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 9.15 9.15 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15026049 10.1016/j.bmcl.2004.01.057 GABA-A receptor; alpha-1/beta-3/gamma-2 1
15026049 10.1016/j.bmcl.2004.01.057 GABA-A receptor; alpha-3/beta-3/gamma-2 1
15026049 10.1016/j.bmcl.2004.01.057 Gamma-aminobutyric acid receptor subunit alpha-2 1
15026049 10.1016/j.bmcl.2004.01.057 Gamma-aminobutyric acid receptor subunit alpha-1 1
15026049 10.1016/j.bmcl.2004.01.057 Gamma-aminobutyric acid receptor subunit alpha-3 1

Data from ChEMBL 36 via Core Engine