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Compound Detail

CHEMBL4547372

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NC1=N[C@H](CC(=O)O)CS1

Basic Information

ChEMBL ID CHEMBL4547372
Phase Preclinical
Structure Type MOL
InChI Key ANCWBXJZUCHVHL-GSVOUGTGSA-N
6
Targets
12
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

160.2
MW (Da)
-0.11
ALogP
4
HBA
2
HBD
75.7
PSA (Ų)
0.59
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 C5H8N2O2S
MW 160.20
Aromatic Rings 0
Heavy Atoms 10
NP-Likeness 0.38

Activity Summary

EC50 10 meas. best 6.92
Ki 2 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 7.23 7.23 58.9 2
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
CHEMBL4523641
EC50 6.92 6.92 120.0 2
Unchecked
CHEMBL612545
EC50 6.43 6.43 370.0 2
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2
CHEMBL4523640
EC50 6.23 5.73 590.0 2
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
EC50 5.82 5.815 1500.0 2
Gamma-aminobutyric acid receptor subunit rho-1
CHEMBL3561
EC50 5.27 5.27 5370.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; anion channel Ki = 59.0 nM 7.23 Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortica... 31117514
GABA-A receptor; anion channel Ki = 58.88 nM 7.23 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 = 120.0 nM 6.92 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 EC50 = 120.23 nM 6.92 Agonist activity at recombinant human GABA-A alpha5beta2gamma2S receptor transie... 31117514
Unchecked EC50 = 370.0 nM 6.43 Agonist activity at recombinant human GABA-A alpha3beta2gamma2S receptor transie... 31117514
Unchecked EC50 = 371.54 nM 6.43 Agonist activity at recombinant human GABA-A alpha3beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 EC50 = 590.0 nM 6.23 Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transie... 31117514
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 1500.0 nM 5.82 Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transie... 31117514
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 1548.82 nM 5.81 Agonist activity at recombinant human GABA-A alpha1beta2gamma2S receptor transie... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 5400.0 nM 5.27 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
Gamma-aminobutyric acid receptor subunit rho-1 EC50 = 5370.32 nM 5.27 Agonist activity at recombinant human GABA-A rho-1 receptor transiently expresse... 31117514
Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 EC50 = 5888.44 nM 5.23 Agonist activity at recombinant human GABA-A alpha4beta2gamma2S receptor transie... 31117514

Literature References

PubMed DOI Target Context # Activities
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit rho-1 3
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2 3
31117514 10.1021/acs.jmedchem.9b00026 Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2 3
31117514 10.1021/acs.jmedchem.9b00026 Unchecked 3
31117514 10.1021/acs.jmedchem.9b00026 GABA-A receptor; alpha-1/beta-2/gamma-2 3
31117514 10.1021/acs.jmedchem.9b00026 GABA-A receptor; anion channel 2
31117514 10.1021/acs.jmedchem.9b00026 No relevant target 1

Data from ChEMBL 36 via Core Engine