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Assay Detail

CHEMBL680644

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity against Gamma-aminobutyric acid A receptor in rat brain synaptosomes after 30 minutes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

A study of 3-amino-N-hydroxypropanesulfonamide derivatives as potential GABAB agonists and their fragmentation to 3-aminopropanesulfinic acid
Ho-Jane Shue, Xiao Chen, Blythin DJ, Carruthers NI, Spitler JM, Shing-Chun Wong, Chapman RW, Rizzo C, West R, She HS
Bioorg Med Chem Lett (1996) 6 : 1709 -1714
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.33 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL545424 1 6.64
CHEMBL553273 1 6.55
CHEMBL149082 TRAMIPROSATE 3.0 1 6.52
CHEMBL32102 HOMOHYPOTAURINE 1 6.33
CHEMBL541547 1 6.21
CHEMBL542848 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL545424 IC50 = 230.0 nM 6.64
CHEMBL553273 IC50 = 280.0 nM 6.55
CHEMBL149082 TRAMIPROSATE IC50 = 300.0 nM 6.52
CHEMBL32102 HOMOHYPOTAURINE IC50 = 470.0 nM 6.33
CHEMBL541547 IC50 = 620.0 nM 6.21
CHEMBL542848 IC50 = 2000.0 nM 5.70