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Assay Detail

CHEMBL2050841

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

Binding
Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptical membrane
10
Total Activities
10
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
Ki 10 6.05 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 7.16
CHEMBL2047401 1 7.10
CHEMBL2047398 1 6.58
CHEMBL2047404 1 6.34
CHEMBL2047403 1 6.14
CHEMBL432748 1 5.89
CHEMBL2047397 1 5.32
CHEMBL2047399 1 5.21
CHEMBL2047405 1 4.70
CHEMBL2047402 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX Ki = 70.0 nM 7.16
CHEMBL2047401 Ki = 80.0 nM 7.10
CHEMBL2047398 Ki = 260.0 nM 6.58
CHEMBL2047404 Ki = 460.0 nM 6.34
CHEMBL2047403 Ki = 720.0 nM 6.14
CHEMBL432748 Ki = 1300.0 nM 5.89
CHEMBL2047397 Ki = 4800.0 nM 5.32
CHEMBL2047399 Ki = 6100.0 nM 5.21
CHEMBL2047405 Ki = 20000.0 nM 4.70
CHEMBL2047402 Ki = 126000.0 nM -