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Assay Detail

CHEMBL749211

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

Binding
In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.
Cordi A, Lacoste JM, Audinot V, Millan M.
Bioorg Med Chem Lett (1999) 9 : 1409 -1414
PubMed 10360746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.14 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL773 GLYCINE 4.0 1 6.60
CHEMBL285123 (D)-SERINE 3.0 1 6.17
CHEMBL283819 1 5.73
CHEMBL286024 1 5.17
CHEMBL771 CYCLOSERINE 4.0 1 5.13
CHEMBL30853 1 4.11
CHEMBL29830 1 4.11
CHEMBL31250 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL773 GLYCINE IC50 = 250.0 nM 6.60
CHEMBL285123 (D)-SERINE IC50 = 670.0 nM 6.17
CHEMBL283819 IC50 = 1870.0 nM 5.73
CHEMBL286024 IC50 = 6800.0 nM 5.17
CHEMBL771 CYCLOSERINE IC50 = 7370.0 nM 5.13
CHEMBL30853 IC50 = 78000.0 nM 4.11
CHEMBL29830 IC50 = 78000.0 nM 4.11
CHEMBL31250 IC50 = 83000.0 nM 4.08