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Compound Detail

CHEMBL72357

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CSc1sc(-c2nc(C)no2)c2c1C(=O)CC(C)(C)C2

Basic Information

ChEMBL ID CHEMBL72357
Phase Preclinical
Structure Type MOL
InChI Key HATOWBRXVGEEIN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
3.98
ALogP
6
HBA
0
HBD
56.0
PSA (Ų)
0.79
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 C14H16N2O2S2
MW 308.43
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -1.16

Activity Summary

Ki 2 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 7.43 7.43 37.0 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 6.73 6.73 185.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12747794 10.1021/jm020582q GABA-A receptor; alpha-5/beta-3/gamma-2 1
12747794 10.1021/jm020582q GABA-A receptor; alpha-1/beta-3/gamma-2 1
12747794 10.1021/jm020582q GABA-A receptor; alpha-2/beta-3/gamma-2 1
12747794 10.1021/jm020582q GABA-A receptor; alpha-3/beta-3/gamma-2 1
12747794 10.1021/jm020582q Gamma-aminobutyric acid receptor subunit alpha-5 1

Data from ChEMBL 36 via Core Engine