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Assay Detail

CHEMBL700297

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

Functional
Ability to block kainate-induced 45 [Ca2+] influx through functional assay of Ionotropic glutamate receptor AMPA activity in rat cerebellar granule cells.
3
Total Activities
2
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

Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.
Welch WM, Ewing FE, Huang J, Menniti FS, Pagnozzi MJ, Kelly K, Seymour PA, Guanowsky V, Guhan S, Guinn MR, Critchett D, Lazzaro J, Ganong AH, DeVries KM, Staigers TL, Chenard BL.
Bioorg Med Chem Lett (2001) 11 : 177 -181
PubMed 11206453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.91 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301759 2 10.00
CHEMBL222519 NBQX 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301759 IC50 = 0.1 nM 10.00
CHEMBL222519 NBQX IC50 = 0.5 nM 9.30
CHEMBL301759 IC50 = 36.0 nM 7.44