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Assay Detail

CHEMBL2050845

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

Binding
Displacement of [3H]kainate from high affinity kainate receptor in rat cortical membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

3-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
Colotta V, Lenzi O, Catarzi D, Varano F, Squarcialupi L, Costagli C, Galli A, Ghelardini C, Pugliese AM, Maraula G, Coppi E, Pellegrini-Giampietro DE, Pedata F, Sabbadin D, Moro S.
Eur J Med Chem (2012) 54 : 470 -482
PubMed 22704999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.91 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047401 1 5.52
CHEMBL2047403 1 5.38
CHEMBL2047398 1 5.16
CHEMBL222519 NBQX 1 5.16
CHEMBL2047404 1 4.76
CHEMBL432748 1 4.72
CHEMBL2047400 1 4.60
CHEMBL2047399 1 4.50
CHEMBL2047397 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047401 IC50 = 3000.0 nM 5.52
CHEMBL2047403 IC50 = 4200.0 nM 5.38
CHEMBL2047398 IC50 = 7000.0 nM 5.16
CHEMBL222519 NBQX IC50 = 7000.0 nM 5.16
CHEMBL2047404 IC50 = 17300.0 nM 4.76
CHEMBL432748 IC50 = 19100.0 nM 4.72
CHEMBL2047400 IC50 = 25000.0 nM 4.60
CHEMBL2047399 IC50 = 32000.0 nM 4.50
CHEMBL2047397 IC50 = 37600.0 nM 4.42