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Assay Detail

CHEMBL870484

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

Binding
Displacement of [3H]muscimol from GABA-A receptor in Sprague-Dawley rat cerebral cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Gelmi ML, Pocar D, Pontremoli G, Pellegrino S, Bombardelli E, Fontana G, Riva A, Balduini W, Carloni S, Cimino M, Johnson F.
J Med Chem (2006) 49 : 5571 -5577
PubMed 16942030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.38 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.62
CHEMBL213907 THIOCOLCHICOSIDE 3.0 1 5.47
CHEMBL213015 1 5.27
CHEMBL213312 1 5.16
CHEMBL215655 1 5.01
CHEMBL214151 1 4.98
CHEMBL386430 1 4.75
CHEMBL438794 1 4.75
CHEMBL213034 1 -
CHEMBL214305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 24.0 nM 7.62
CHEMBL213907 THIOCOLCHICOSIDE IC50 = 3400.0 nM 5.47
CHEMBL213015 IC50 = 5400.0 nM 5.27
CHEMBL213312 IC50 = 7000.0 nM 5.16
CHEMBL215655 IC50 = 9700.0 nM 5.01
CHEMBL214151 IC50 = 10500.0 nM 4.98
CHEMBL386430 IC50 = 17700.0 nM 4.75
CHEMBL438794 IC50 = 18000.0 nM 4.75
CHEMBL213034 IC50 > 100000.0 nM -
CHEMBL214305 IC50 > 100000.0 nM -