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Compound Detail

CHEMBL4081736

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O=c1c(-c2ccsc2)c[nH]c2c(-c3ccccn3)cnn12

Basic Information

ChEMBL ID CHEMBL4081736
Phase Preclinical
Structure Type MOL
InChI Key AMPDVLJTHKQJOP-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

294.3
MW (Da)
2.81
ALogP
5
HBA
1
HBD
63.0
PSA (Ų)
0.62
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 C15H10N4OS
MW 294.34
Aromatic Rings 4
Heavy Atoms 21
NP-Likeness -1.91

Activity Summary

Ki 4 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.41 8.41 3.9 1
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL343
Ki 8.15 8.15 7.0 1
Gamma-aminobutyric acid receptor subunit alpha-5
CHEMBL300
Ki 6.13 6.13 740.0 1
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL341
Ki 6.03 6.03 927.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27894044 10.1016/j.ejmech.2016.11.019 Unchecked 3
27894044 10.1016/j.ejmech.2016.11.019 Gamma-aminobutyric acid receptor subunit alpha-1 1
27894044 10.1016/j.ejmech.2016.11.019 Gamma-aminobutyric acid receptor subunit alpha-2 1
27894044 10.1016/j.ejmech.2016.11.019 Gamma-aminobutyric acid receptor subunit alpha-5 1

Data from ChEMBL 36 via Core Engine