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Assay Detail

CHEMBL4219620

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

Binding
Positive allosteric modulation of human glycine alpha1beta receptor expressed in HEK293T cells assessed as glycine-induced increase in current response after 18 to 24 hrs by membrane potential blue dye based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Glycine receptor (alpha-1/beta) (CHEMBL2363052)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Sparling BA, DiMauro EF.
Bioorg Med Chem Lett (2017) 27 : 3207 -3218
PubMed 28606760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.29 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4070615 1 7.80
CHEMBL4074873 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4070615 EC50 = 16.0 nM 7.80
CHEMBL4074873 EC50 = 171.0 nM 6.77