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Assay Detail

CHEMBL4219942

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

Binding
Positive allosteric modulation of human GlyRalpha3beta expressed in CHO cells assessed as potentiation of EC20 glycine-induced ion flux by HT assay
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glycine receptor alpha-3/beta (CHEMBL4106144)
Type PROTEIN COMPLEX
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
pEC50 5 - -
EC50 4 6.11 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4227298 1 7.87
CHEMBL4227048 1 6.18
CHEMBL4228024 1 5.40
CHEMBL4225948 1 4.99
CHEMBL4226202 1 -
CHEMBL4226258 1 -
CHEMBL1331986 1 -
CHEMBL4066349 1 -
CHEMBL281071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4227298 EC50 = 13.49 nM 7.87
CHEMBL4227048 EC50 = 660.69 nM 6.18
CHEMBL4228024 EC50 = 3981.07 nM 5.40
CHEMBL4225948 EC50 = 10232.93 nM 4.99
CHEMBL4226202 pEC50 - -
CHEMBL4226258 pEC50 - -
CHEMBL1331986 pEC50 - -
CHEMBL4066349 pEC50 - -
CHEMBL281071 pEC50 - -