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Assay Detail

CHEMBL749367

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

Binding
Inhibition of [3H]MDL-105,519 binding to NMDA receptor glycine-binding site
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists.
Auberson YP, Acklin P, Allgeier H, Biollaz M, Bischoff S, Ofner S, Veenstra SJ.
Bioorg Med Chem Lett (1998) 8 : 71 -74
PubMed 9871631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.89 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540084 1 9.47
CHEMBL163000 1 7.52
CHEMBL162757 1 7.30
CHEMBL349778 1 6.92
CHEMBL552793 1 6.92
CHEMBL556379 1 6.39
CHEMBL553402 1 6.30
CHEMBL544884 1 6.14
CHEMBL162066 1 6.12
CHEMBL536244 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540084 IC50 = 0.34 nM 9.47
CHEMBL163000 IC50 = 30.0 nM 7.52
CHEMBL162757 IC50 = 50.0 nM 7.30
CHEMBL349778 IC50 = 120.0 nM 6.92
CHEMBL552793 IC50 = 120.0 nM 6.92
CHEMBL556379 IC50 = 410.0 nM 6.39
CHEMBL553402 IC50 = 500.0 nM 6.30
CHEMBL544884 IC50 = 720.0 nM 6.14
CHEMBL162066 IC50 = 750.0 nM 6.12
CHEMBL536244 IC50 = 1400.0 nM 5.85