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Assay Detail

CHEMBL4219947

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

Binding
Positive allosteric modulation of GlyRalpha1 (unknown origin) assessed as potentiation of glycine-induced response
4
Total Activities
4
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

Glycine receptor subunit alpha-1 (CHEMBL5845)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
Cioffi CL.
J Med Chem (2018) 61 : 2652 -2679
PubMed 28876062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 9.80 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228372 1 10.22
CHEMBL4227297 1 9.37
CHEMBL4227144 1 -
CHEMBL4226150 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228372 EC50 = 0.06 nM 10.22
CHEMBL4227297 EC50 = 0.43 nM 9.37
CHEMBL4227144 EC50 = 0.00016 nM -
CHEMBL4226150 EC50 = 0.0012 nM -