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Assay Detail

CHEMBL752334

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

Binding
Inhibition of binding of [3H]glycine to N-methyl-D-aspartate glutamate receptor 1 from crude synaptic membranes prepared from adult rat cerebral cortex.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists.
Balsamini C, Bedini A, Diamantini G, Spadoni G, Tontini A, Tarzia G, Di Fabio R, Feriani A, Reggiani A, Tedesco G, Valigi R.
J Med Chem (1998) 41 : 808 -820
PubMed 9526557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31741 1 8.70
CHEMBL58663 1 8.22
CHEMBL287327 1 8.11
CHEMBL114610 1 7.89
CHEMBL22895 1 7.50
CHEMBL31344 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31741 IC50 = 2.0 nM 8.70
CHEMBL58663 IC50 = 6.0 nM 8.22
CHEMBL287327 IC50 = 7.8 nM 8.11
CHEMBL114610 IC50 = 13.0 nM 7.89
CHEMBL22895 IC50 = 32.0 nM 7.50
CHEMBL31344 IC50 = 140.0 nM 6.85