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Assay Detail

CHEMBL4029945

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

Binding
Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gamma-aminobutyric acid type B receptor subunit 1 (CHEMBL2064)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
Johnstone S, Albert JS.
Bioorg Med Chem Lett (2017) 27 : 2239 -2258
PubMed 28408223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.10 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392394 GS-39783 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392394 GS-39783 EC50 = 79.43 nM 7.10