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Compound Detail

CHEMBL4204097

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CCCCOc1ccc(C(=O)Nc2c(-c3cccs3)nc3c(Br)cc(Br)cn23)cc1

Basic Information

ChEMBL ID CHEMBL4204097
Phase Preclinical
Structure Type MOL
InChI Key UEVAWVLUFSBGAY-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

549.3
MW (Da)
7.02
ALogP
5
HBA
1
HBD
55.6
PSA (Ų)
0.25
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19Br2N3O2S
MW 549.29
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.65

Activity Summary

IC50 3 meas. best 6.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/delta
CHEMBL4296053
IC50 6.07 6.07 860.0 1
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3
CHEMBL4296052
IC50 5.6 5.6 2500.0 1
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
CHEMBL4296054
IC50 5.26 5.26 5510.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29451785 10.1021/acs.jmedchem.7b01484 Gamma-aminobutyric acid receptor subunit alpha-6/beta-3 2
29451785 10.1021/acs.jmedchem.7b01484 Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/delta 2
29451785 10.1021/acs.jmedchem.7b01484 Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2 2

Data from ChEMBL 36 via Core Engine