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Assay Detail

CHEMBL749333

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

Binding
In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]CGS-19,755 ligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action.
Ornstein PL, Schoepp DD, Arnold MB, Leander JD, Lodge D, Paschal JW, Elzey T.
J Med Chem (1991) 34 : 90 -97
PubMed 1825117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.24 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39664 SELFOTEL 2.0 1 7.27
CHEMBL173031 1 6.97
CHEMBL366591 1 6.11
CHEMBL173032 1 5.64
CHEMBL362277 1 5.23
CHEMBL444616 1 -
CHEMBL178746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39664 SELFOTEL IC50 = 54.0 nM 7.27
CHEMBL173031 IC50 = 107.0 nM 6.97
CHEMBL366591 IC50 = 777.0 nM 6.11
CHEMBL173032 IC50 = 2280.0 nM 5.64
CHEMBL362277 IC50 = 5830.0 nM 5.23
CHEMBL444616 IC50 > 10000.0 nM -
CHEMBL178746 IC50 > 10000.0 nM -