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Assay Detail

CHEMBL699741

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

Functional
Antagonistic activity against Ionotropic glutamate receptor AMPA using kainate-evoked current in Xenopus oocytes injected with rat brain mRNA
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.
Pratt J, Jimonet P, Bohme GA, Boireau A, Damour D, Debono MW, Genevois-Borella A, Randle JC, Ribeill Y, Stutzmann JM, Vuilhorgne M, Mignani S.
Bioorg Med Chem Lett (2000) 10 : 2749 -2754
PubMed 11133083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.74 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24980 1 8.30
CHEMBL433424 1 7.64
CHEMBL277281 1 7.54
CHEMBL222519 NBQX 1 7.51
CHEMBL418952 1 7.28
CHEMBL93287 1 6.98
CHEMBL329639 1 6.67
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 6.64
CHEMBL13260 YM-90K 1 6.58
CHEMBL279116 1 5.75
CHEMBL93902 1 5.70
CHEMBL91509 1 5.58
CHEMBL329778 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24980 IC50 = 5.0 nM 8.30
CHEMBL433424 IC50 = 23.0 nM 7.64
CHEMBL277281 IC50 = 29.0 nM 7.54
CHEMBL222519 NBQX IC50 = 31.0 nM 7.51
CHEMBL418952 IC50 = 53.0 nM 7.28
CHEMBL93287 IC50 = 104.0 nM 6.98
CHEMBL329639 IC50 = 214.0 nM 6.67
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 230.0 nM 6.64
CHEMBL13260 YM-90K IC50 = 260.0 nM 6.58
CHEMBL279116 IC50 = 1800.0 nM 5.75
CHEMBL93902 IC50 = 2008.0 nM 5.70
CHEMBL91509 IC50 = 2644.0 nM 5.58
CHEMBL329778 IC50 = 3252.0 nM 5.49