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Assay Detail

CHEMBL919854

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

Binding
Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat spinal cord brainstem membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brainstem
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors.
Gelmi ML, Fontana G, Pocar D, Pontremoli G, Pellegrino S, Bombardelli E, Riva A, Balduini W, Carloni S, Cimino M.
J Med Chem (2007) 50 : 2245 -2248
PubMed 17411024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.51 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.82
CHEMBL213907 THIOCOLCHICOSIDE 3.0 1 5.72
CHEMBL390287 1 5.70
CHEMBL223911 1 5.60
CHEMBL388974 1 5.46
CHEMBL376390 1 5.40
CHEMBL274560 1 5.38
CHEMBL227024 1 5.37
CHEMBL390393 1 5.30
CHEMBL426751 1 5.23
CHEMBL390587 1 5.11
CHEMBL228245 1 5.10
CHEMBL390346 1 5.09
CHEMBL390948 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 15.0 nM 7.82
CHEMBL213907 THIOCOLCHICOSIDE IC50 = 1900.0 nM 5.72
CHEMBL390287 IC50 = 2000.0 nM 5.70
CHEMBL223911 IC50 = 2500.0 nM 5.60
CHEMBL388974 IC50 = 3500.0 nM 5.46
CHEMBL376390 IC50 = 4000.0 nM 5.40
CHEMBL274560 IC50 = 4200.0 nM 5.38
CHEMBL227024 IC50 = 4300.0 nM 5.37
CHEMBL390393 IC50 = 5000.0 nM 5.30
CHEMBL426751 IC50 = 5900.0 nM 5.23
CHEMBL390587 IC50 = 7800.0 nM 5.11
CHEMBL228245 IC50 = 8000.0 nM 5.10
CHEMBL390346 IC50 = 8200.0 nM 5.09
CHEMBL390948 IC50 = 14200.0 nM 4.85