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Compound Detail

CHEMBL173219

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COC(=O)c1cc2c3cc(SC#N)ccc3nc-2c[nH]1

Basic Information

ChEMBL ID CHEMBL173219
Phase Preclinical
Structure Type MOL
InChI Key FLTICUPGYVYGAM-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

283.3
MW (Da)
3.03
ALogP
5
HBA
1
HBD
78.8
PSA (Ų)
0.44
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 C14H9N3O2S
MW 283.31
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.91

Activity Summary

Ki 3 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
Ki 8.47 8.47 3.4 1
GABA-A receptor; alpha-3/beta-3/gamma-2
CHEMBL2094120
Ki 7.52 7.52 30.0 1
GABA-A receptor; alpha-5/beta-3/gamma-2
CHEMBL2094122
Ki 6.85 6.85 141.0 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

Data from ChEMBL 36 via Core Engine