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Assay Detail

CHEMBL679649

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

Binding
Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Brain membranes
Confidence 7 — Homologous single protein target
Curated By Expert

Target

GABA B receptor (CHEMBL2111474)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis and activity of 5-(aminomethylene)-1,3-cyclohexanediones: enolic analogues of gamma-aminobutyric acid.
Mann A, Humblet C, Chambon JP, Schlichter R, Desarmenien M, Feltz P, Wermuth CG.
J Med Chem (1985) 28 : 1440 -1446
PubMed 2995665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.22 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL701 BACLOFEN 4.0 1 7.22
CHEMBL277498 NIPECOTIC ACID 1 -
CHEMBL32861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL701 BACLOFEN IC50 = 60.0 nM 7.22
CHEMBL277498 NIPECOTIC ACID IC50 > 100000.0 nM -
CHEMBL32861 IC50 > 100000.0 nM -