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Assay Detail

CHEMBL681130

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

Binding
Displacement of [3H]gamma-aminobutyric acid from sodium-independent Gamma-aminobutyric acid (GABA-A) receptor synaptic membrane binding sites from rat brain tissue
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid.
O'Donnell JP, Johnson DA, Azzaro AJ.
J Med Chem (1980) 23 : 1142 -1144
PubMed 7420361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.10 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 8.49
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.70
CHEMBL14964 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273481 MUSCIMOL IC50 = 3.2 nM 8.49
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 20.0 nM 7.70
CHEMBL14964 IC50 = 290000.0 nM -