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Assay Detail

CHEMBL783636

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

Functional
Inhibition of 40 uM AMPA induced depolarizations in a rat cortical slice.
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 12 4.76 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16315 2 5.75
CHEMBL16303 3 4.87
CHEMBL16360 1 4.82
CHEMBL279120 1 4.81
CHEMBL16261 1 4.56
CHEMBL17098 1 4.36
CHEMBL16342 1 4.11
CHEMBL16589 1 -
CHEMBL279648 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16315 IC50 = 1800.0 nM 5.75
CHEMBL16315 IC50 = 6000.0 nM 5.22
CHEMBL16303 IC50 = 13400.0 nM 4.87
CHEMBL16303 IC50 = 14900.0 nM 4.83
CHEMBL16360 IC50 = 15000.0 nM 4.82
CHEMBL279120 IC50 = 15500.0 nM 4.81
CHEMBL16261 IC50 = 27300.0 nM 4.56
CHEMBL17098 IC50 = 43300.0 nM 4.36
CHEMBL16303 IC50 = 58700.0 nM 4.23
CHEMBL16342 IC50 = 77400.0 nM 4.11
CHEMBL16589 IC50 > 100000.0 nM -
CHEMBL279648 IC50 > 100000.0 nM -