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Assay Detail

CHEMBL644177

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

Binding
Inhibition of [3H]AMPA binding to AMPA receptor of rat brain membranes.
21
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Structure-activity studies of aryl-spaced decahydroisoquinoline-3-carboxylic acid ampa receptor antagonists
Bleisch TJ, Ornstein PL, Allen NK, Wright RA, Lodge D, Schoepp DD
Bioorg Med Chem Lett (1997) 7 : 1161 -1166
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.08 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16303 3 5.89
CHEMBL16315 2 5.85
CHEMBL16261 1 5.37
CHEMBL17098 1 5.37
CHEMBL16360 1 5.21
CHEMBL279120 1 4.66
CHEMBL435755 1 4.33
CHEMBL280498 1 4.17
CHEMBL16289 1 -
CHEMBL16944 1 -
CHEMBL16243 1 -
CHEMBL280054 1 -
CHEMBL279527 1 -
CHEMBL279648 1 -
CHEMBL417625 1 -
CHEMBL16589 1 -
CHEMBL16342 1 -
CHEMBL274226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16303 IC50 = 1300.0 nM 5.89
CHEMBL16315 IC50 = 1400.0 nM 5.85
CHEMBL16303 IC50 = 3200.0 nM 5.50
CHEMBL17098 IC50 = 4300.0 nM 5.37
CHEMBL16261 IC50 = 4300.0 nM 5.37
CHEMBL16315 IC50 = 4800.0 nM 5.32
CHEMBL16360 IC50 = 6100.0 nM 5.21
CHEMBL279120 IC50 = 22000.0 nM 4.66
CHEMBL435755 IC50 = 46800.0 nM 4.33
CHEMBL16303 IC50 = 55400.0 nM 4.26
CHEMBL280498 IC50 = 66900.0 nM 4.17
CHEMBL16944 IC50 > 100000.0 nM -
CHEMBL417625 IC50 > 100000.0 nM -
CHEMBL274226 IC50 > 100000.0 nM -
CHEMBL16342 IC50 > 100000.0 nM -
CHEMBL16589 IC50 > 100000.0 nM -
CHEMBL279648 IC50 > 100000.0 nM -
CHEMBL279527 IC50 > 100000.0 nM -
CHEMBL280054 IC50 > 100000.0 nM -
CHEMBL16243 IC50 > 100000.0 nM -
CHEMBL16289 IC50 > 100000.0 nM -