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Assay Detail

CHEMBL745044

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

Binding
Binding affinity against NMDA receptor using [3H]-CGS- 19755 as a radioligand in rat
7
Total Activities
5
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

(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.
Ornstein PL, Arnold MB, Allen NK, Leander JD, Tizzano JP, Lodge D, Schoepp DD.
J Med Chem (1995) 38 : 4885 -4890
PubMed 8523401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.38 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72123 1 6.09
CHEMBL308941 3 6.00
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 4.58
CHEMBL423201 1 4.42
CHEMBL144462 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72123 IC50 = 820.0 nM 6.09
CHEMBL308941 IC50 = 1000.0 nM 6.00
CHEMBL308941 IC50 = 1600.0 nM 5.80
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 26400.0 nM 4.58
CHEMBL423201 IC50 = 38400.0 nM 4.42
CHEMBL308941 IC50 > 100000.0 nM -
CHEMBL144462 IC50 > 100000.0 nM -