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Assay Detail

CHEMBL750508

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

Binding
Affinity of [3H]-CGS- 19755 radioligand to rat N-methyl-D-aspartate (NMDA) receptor
30
Total Activities
24
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

Structure-activity studies of 6-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity.
Ornstein PL, Arnold MB, Allen NK, Bleisch T, Borromeo PS, Lugar CW, Leander JD, Lodge D, Schoepp DD.
J Med Chem (1996) 39 : 2232 -2244
PubMed 8667366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 4.39 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 2 4.92
CHEMBL309342 2 4.74
CHEMBL70773 2 4.53
CHEMBL72573 1 4.36
CHEMBL71755 3 4.22
CHEMBL71167 1 4.21
CHEMBL73837 1 4.21
CHEMBL73356 1 -
CHEMBL311632 1 -
CHEMBL71043 1 -
CHEMBL423498 2 -
CHEMBL307281 1 -
CHEMBL72413 1 -
CHEMBL73072 1 -
CHEMBL440493 1 -
CHEMBL70937 1 -
CHEMBL422589 1 -
CHEMBL72592 1 -
CHEMBL433294 1 -
CHEMBL70535 1 -
CHEMBL72544 1 -
CHEMBL306851 1 -
CHEMBL307562 1 -
CHEMBL304282 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 12100.0 nM 4.92
CHEMBL309342 IC50 = 18100.0 nM 4.74
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 26400.0 nM 4.58
CHEMBL70773 IC50 = 29800.0 nM 4.53
CHEMBL309342 IC50 = 29400.0 nM 4.53
CHEMBL72573 IC50 = 43900.0 nM 4.36
CHEMBL70773 IC50 = 47900.0 nM 4.32
CHEMBL71755 IC50 = 60600.0 nM 4.22
CHEMBL71167 IC50 = 60900.0 nM 4.21
CHEMBL73837 IC50 = 61800.0 nM 4.21
CHEMBL71755 IC50 = 76900.0 nM 4.11
CHEMBL71755 IC50 = 99200.0 nM 4.00
CHEMBL71043 IC50 > 10000.0 nM -
CHEMBL440493 IC50 > 10000.0 nM -
CHEMBL73356 IC50 > 10000.0 nM -
CHEMBL72413 IC50 > 100000.0 nM -
CHEMBL423498 IC50 > 100000.0 nM -
CHEMBL304282 IC50 > 100000.0 nM -
CHEMBL70937 IC50 > 100000.0 nM -
CHEMBL311632 IC50 > 100000.0 nM -
CHEMBL72592 IC50 > 10000.0 nM -
CHEMBL307281 IC50 > 100000.0 nM -
CHEMBL433294 IC50 > 100000.0 nM -
CHEMBL73072 IC50 > 10000.0 nM -
CHEMBL70535 IC50 > 100000.0 nM -
CHEMBL72544 IC50 > 100000.0 nM -
CHEMBL306851 IC50 > 100000.0 nM -
CHEMBL307562 IC50 > 100000.0 nM -
CHEMBL423498 IC50 > 100000.0 nM -
CHEMBL422589 IC50 > 100000.0 nM -