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Assay Detail

CHEMBL749985

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

Binding
Displacement of [3H]TCP from the TCP site of NMDA receptor in rat brain homogenate
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Excellent acceleration of the Diels-Alder reaction by microwave irradiation for the synthesis of new fluorine-substituted ligands of NMDA receptor.
Sasaki S, Ishibashi N, Kuwamura T, Sano H, Matoba M, Nisikawa T, Maeda M.
Bioorg Med Chem Lett (1998) 8 : 2983 -2986
PubMed 9873659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.02 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317637 1 8.44
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.33
CHEMBL317531 2 7.33
CHEMBL101120 2 7.21
CHEMBL99960 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317637 IC50 = 3.6 nM 8.44
CHEMBL275528 PHENCYCLIDINE IC50 = 47.0 nM 7.33
CHEMBL317531 IC50 = 47.0 nM 7.33
CHEMBL101120 IC50 = 61.0 nM 7.21
CHEMBL317531 IC50 = 89.0 nM 7.05
CHEMBL101120 IC50 = 141.0 nM 6.85
CHEMBL99960 IC50 = 12360.0 nM 4.91