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Compound Detail

CHEMBL4464494

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CC(C(=O)O)C1CSC(N)=N1

Basic Information

ChEMBL ID CHEMBL4464494
Phase Preclinical
Structure Type MOL
InChI Key HQCCRLRYTXVTRA-UHFFFAOYSA-N
6
Targets
18
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

174.2
MW (Da)
0.14
ALogP
4
HBA
2
HBD
75.7
PSA (Ų)
0.62
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C6H10N2O2S
MW 174.22
Aromatic Rings 0
Heavy Atoms 11
NP-Likeness 0.49

Activity Summary

EC50 14 meas. best 5.92
Ki 4 meas. best 6.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 6.49 6.1925 323.6 4
Gamma-aminobutyric acid receptor subunit rho-1
CHEMBL3561
EC50 5.92 5.525 1200.0 4
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
CHEMBL4523641
EC50 5.57 5.265 2691.5 4
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
EC50 4.6 4.6 25000.0 2
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2
CHEMBL4523640
EC50 4.58 4.58 26000.0 2
Unchecked
CHEMBL612545
EC50 4.52 4.52 30000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; anion channel Ki = 323.59 nM 6.49 Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortica... 31117514
GABA-A receptor; anion channel Ki = 330.0 nM 6.48 Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortica... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 1202.26 nM 5.92 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 1200.0 nM 5.92 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
GABA-A receptor; anion channel Ki = 1230.27 nM 5.91 Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortica... 31117514
GABA-A receptor; anion channel Ki = 1300.0 nM 5.89 Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortica... 31117514
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 EC50 = 2691.53 nM 5.57 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 EC50 = 2700.0 nM 5.57 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 7413.1 nM 5.13 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 7400.0 nM 5.13 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 EC50 = 11000.0 nM 4.96 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 EC50 = 10964.78 nM 4.96 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 25000.0 nM 4.6 Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transie... 31117514
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 25118.86 nM 4.6 Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 EC50 = 26000.0 nM 4.58 Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 EC50 = 26302.68 nM 4.58 Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transie... 31117514
Unchecked EC50 = 30000.0 nM 4.52 Agonist activity at recombinant human GABA-A alpha3beta2gamma2S receptor transie... 31117514
Unchecked EC50 = 30199.52 nM 4.52 Agonist activity at recombinant human GABA-A alpha3beta2gamma2S receptor transie... 31117514

Literature References

PubMed DOI Target Context # Activities
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 7
31117514 10.1021/acs.jmedchem.9b00026 Unchecked 7
31117514 10.1021/acs.jmedchem.9b00026 GABA-A receptor; alpha-1/beta-2/gamma-2 7
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit rho-1 6
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 6
31117514 10.1021/acs.jmedchem.9b00026 GABA-A receptor; anion channel 4
31117514 10.1021/acs.jmedchem.9b00026 Sodium- and chloride-dependent GABA transporter 1 4
31117514 10.1021/acs.jmedchem.9b00026 Sodium- and chloride-dependent GABA transporter 2 4
31117514 10.1021/acs.jmedchem.9b00026 Sodium- and chloride-dependent GABA transporter 3 4
31117514 10.1021/acs.jmedchem.9b00026 Sodium- and chloride-dependent betaine transporter 4

Data from ChEMBL 36 via Core Engine