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Assay Detail

CHEMBL4481497

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

Binding
Displacement of [3H]NCS382 from high-affinity GHB binding site of alpha4betadelta receptor in mouse brain membranes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular Membranes
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
Krall J, Bavo F, Falk-Petersen CB, Jensen CH, Nielsen JO, Tian Y, Anglani V, Kongstad KT, Piilgaard L, Nielsen B, Gloriam DE, Kehler J, Jensen AA, Harpsøe K, Wellendorph P, Frølund B.
J Med Chem (2019) 62 : 2798 -2813
PubMed 30763084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.80 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32503 GABAZINE 1 4.80
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32503 GABAZINE Ki = 16000.0 nM 4.80
CHEMBL96 GAMMA-AMINOBUTYRIC ACID Ki = 2100000.0 nM -